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| Dr.
Wilbur R. Leopold, Ph.D |
| President
and Chief Executive Officer, MIR Preclinical Services |
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Career
Synopsis |
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Extensive
formal training in engineering, organic and inorganic
synthesis, biochemistry, toxicology, and pharmacology
of anticancer drugs.
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Principal
scientist and program leader for the discovery and/or
development of more than 15 anticancer agents that
advanced to clinical trial. Several of these are
now marketed (Amsacrine, Trimetrexate, Nipent), and
others remain in development [CI-994 (HDAC inhibitor);
CI-1033 (erbB inactivator); CI-1040 (MEK inhibitor);
anthrapyrazoles (topo II inhibitors). Compounds taken
to clinical trial represent a diverse spectrum of
mechanistic classes including: antifolates, tubulin
binders, topoismerase I and II inhibitors, platinum
coordination complexes, nucleoside analogs, histone
deacetylase inhibitors, alkylating agents, DNA polymerase
inhibitors, natural products, DNA repair inhibitors
(PARP), electron affinic radiation sensitizers, polyamine
disregulators, adenosine deaminase inhibitors, erbB
kinase inhibitors, antiangiogenics (VEGF/bFGF receptor
kinase inhibitors), a MEK inhibitor, and a tumor
specific virus .
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In
1989, after assuming the leadership role for the
Parke-Davis anticancer drug discovery program, initiated
and led the retooling of the discovery effort to
focus exclusively on novel molecular targets elucidated
by recent advances in the molecular understanding
of the genetics of oncogenes and tumor suppressor
genes. The quality of this effort has been well recognized
with publications in Science, PNAS, and Nature Medicine
on several of our more recent clinical candidates.
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Led
the growth of the cancer drug discovery effort at
Parke-Davis/Pfizer to its current status as one of
the largest therapeutic areas in the company. The
discovery effort employed more than 120 FTEs at the
Ann Arbor campus.
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In
light of the switch to a discovery strategy based
on specific molecular targets, spearheaded the application
of pharmacodynamic assays to the drug discovery process.
This led to dramatically increased throughput in
the in vivo laboratories, and more precise estimation
of dosing protocols for subsequent clinical trials.
It is now rare for an exploratory project to receive
synthetic chemistry support if in vitro and in vivo
pharmacodynamic assays are not available.
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Completely
automated data collection for the in vivo drug evaluation
(Experimental Oncology) laboratories. Efficiency
studies indicate a >50% saving in total FTEs.
All data collection is computer based, with data
automatically logged into an Inquire database. The
system provides immediate access to all data by any
scientist working on the project. Calculations for
drug dilutions are automatically printed at the beginning
of each day based on current animal census and body
weights for each group in every experiment, and labels
for dosing bottles are automatically printed. All
calculations and tables for interim or final reports
are automatically performed via interactive software.
Animal census is also automatically tracked, as are
drug inventories and tumor passage records.
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Spearheaded
the use of high throughput gene expression profiling
for quality control of the Parke-Davis tumor bank,
and for the evaluation of new, hopefully more predictive
tumor models.
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Chaired
the clinical development teams (Phase I and II) for
our first two mechanistically novel agents; CI-1006
(a polyamine analog designed to induce a homeostatic
response to perceived polyamine excess), and CI-1033
(an extraordinarily potent and selective irreversible
inactivator of the entire EGF receptor family of
oncogenic tyrosine kinases).
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Initiated
a gene therapy discovery program via research collaboration
with Onyx Pharmaceuticals, based on an E1B deficient
adenovirus vector. This vector allows replication
only in functionally p53-deficient cells (tumor cells)
and is expected to provide tumor specific gene expression,
potent bystander effects, and extremely high transgene
expression levels. Two discovery programs based on
this vector are underway, one to deliver a prodrug
converting enzyme and another to deliver a transgene
that will stimulate an immune response to the tumor.
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Stepped
down as Executive Director of Cancer Discovery at
Pfizer in 2002 to refocus efforts more closely on
issues of cancer drug discovery, and less on administrative
issues associated with cross-therapeutic area functions.
Initiated new methods for automation of preclinical
pharmacodynamic assays to keep pace with recent advances
in chemical synthesis throughput.
- Selected
current or recent administrative responsibilities:
- President
and CEO, Molecular Imaging research, Inc.
- Adjunct
Professor of Medicinal Chemistry, University
of Michigan
- Senior
Director of Cancer Pharmacology
- Chair
of the Oncology Biomarker Utilization Strategy
Team
- Ann
Arbor Site Leader for Pfizer Oncology Drug Discovery
- Chair
of Cancer Discovery Team
- Co-Chair
of Pfizer Oncology Integration Team
- Member
of the Due Diligence Team for the Agouron Acquisition
by Parke-Davis
- Co-Chair
of Parke-Davis/Agouron Integration Team
- Charter
Member of Expression Profiling Review Committee
- Chair
of CI-1006 Clinical Development Team
- Chair
of CI-1033 Clinical Development Team
- Chair
of Parke-Davis/Onyx Cell Cycle Collaboration
Research Management Committee
- Chair
of Parke-Davis/Onyx Gene Therapy Collaboration
Research Management Committee
- Member
of the Pfizer Ann Arbor Biology Leadership Team
- Member
of the Pfizer Ann Arbor Discovery Leadership
Forum
- Member
of the Purdue Cancer Center External Advisory
Committee
- Member
of the University of Michigan Cancer Center’s
Research Committee
- Member
of the Piedmont Research Center Scientific Advisory
Board
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Professional
Resume |
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EDUCATION: |
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University
of Wisconsin Medical School, Ph.D., Oncology, 1981.
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Major
Professors: Drs. James and Elizabeth Miller, McArdle Laboratory
for Cancer Research
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Minor:
Chemistry
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Thesis:
Carcinogenic, Mutagenic, and Biochemical Properties of
Platinum Antitumor Coordination Complexes and of S-Vinyl-
and S-Ethyl-Homocystein
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University
of Illinois, M.S., Biochemistry, 1973.
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University
of Illinois, B.S., Chemical Engineering, 1971.
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PROFESSIONAL
POSITIONS: |
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President and CEO,
MIR Preclinical Services 2006 – present.
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President,
MIR Preclinical Services 2003 – 2006.
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Senior
Director, Cancer Pharmacology, Pfizer Ann Arbor Laboratories.
2002 – 2003.
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Executive
Director and Site Leader Cancer Discovery, Pfizer Ann Arbor
Laboratories. 2000-2002.
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Senior
Director of Cancer Research, Experimental Therapy Department,
Parke-Davis and Pfizer Research. 1994-2000.
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Director
of Cancer Research, Experimental Therapy Department, Parke-Davis
Research. 1990-1994.
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Section
Director - Tumor Biology, Pharmacology Department, Parke-Davis
Research. 1988-1990.
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Senior
Research Associate - Chemotherapy Department, Head - Tumor
Biology, Parke-Davis Research. 1986-1988.
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Research
Associate - Chemotherapy Department, Head - Experimental
Oncology Group, Parke-Davis Research. 1985-1986.
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Senior
Scientist - Chemotherapy Department, Head - Experimental
Oncology Group, Parke-Davis Research. 1983-1985.
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Scientist
- Chemotherapy Department, Head - Experimental Oncology
Group, Parke-Davis Research, 1982-1983.
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Research
Toxicologist - Proposal Preparation and Study Cost Analysis,
Southern Research Institute, Toxicology Division. 1982.
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Research
Oncologist - Experimental Chemotherapy and Tumor Biology,
Southern Research Institute, Chemotherapy Division. 1981-1982.
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Exxon
Company U.S.A., Energy Conservation and Pollution Control
Section - Process Engineering Department, Process Design
and Cost Analysis, 1974-1975.
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Exxon
Company U.S.A., Cracking Section - Process Engineering
Department, Technical Services and Plant Optimization,
1973-1974.
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Exxon
Company U.S.A., Mathematics and Computing Department, Computer
Applications for Process Control, 1971-1972.
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A.
E. Staley Manufacturing Co., Dextrose and Syrup Refinery,
Plant Optimization Studies, June 1970 - September 1970.
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CONSULTING: |
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Adjunct
Professor of Medicinal Chemistry, University of Michigan 2005-present.
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Member - RAID Special Emphasis Panel, Developmental Therapeutics Program, NCI 2006-present.
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Consultant
for NCI/DTP – Principles of Efficient Drug Discovery,
December 8, 2004.
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Member
– Scientific Advisory Board, Sagres Discovery, Inc.
2003
– 2004.
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Member
- University of Michigan Cancer Research Committee - 1995-present.
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Adjunct
Professor of Medicinal Chemistry, University of Michigan.
2003-present.
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Member
External Advisory Board – Purdue University Cancer
Center - 1997-present.
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Member
of the Piedmont Research Center Scientific Advisory Board –
1999-2003.
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Consultant/Reviewer
- NCDDG Review, NCI, Jan. 24-26, 1995.
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Consultant
for NCI, "Ad Hoc In Vivo Workshop" and status
of the NCI Tumor Panel on the development of in vivo testing
strategies. May 7-8, 1992.
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Consultant
for NCI, Developmental Therapeutics Program Workshop on "Molecular
Targets for the Discovery of New Anticancer Therapies."
Nov. 12-13, 1991.
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Reviewer
For: |
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Cell
Growth and Differentiation, – 1997-present
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Clinical
Cancer Research, 1994 - present
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J.
Cell. Biochem., 1990 - present.
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Cancer
Chemotherapy and Pharmacology, 1986 - present.
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Cancer
Research, 1984 - present.
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Clinical
Cancer Research 2001-present.
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Consultant/Reviewer
- Experimental Therapeutics Study Section Two - Small Business
Innovative Research Program, NIH, March 30, 1988.
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Experimental
Therapeutics Study Section One, NIH, Oct. 21-24, 1986.
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Professional
Societies: |
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American
Association for Cancer Research
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American
Society for Clinical Oncology
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American
Association for the Advancement of Science
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American
Chemical Society
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HONORS: |
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Patents: |
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- Method
for Treating Neoplasms. E.F. Elslager and W.R. Leopold. US
Patent 4853221, August 1, 1989.
- Treatment
of Prostate Cancer. W.R. Grove and W.R. Leopold. US Patent
5569667, October 29, 1996.
- Treatment
of Renal Cell Carcinoma. W.R. Grove, W.R. Leopold, P. Lorusso,
M. Meyer. US Patent Pending.
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Publications: |
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- S-vinylhomocysteine,
an Analog of Ethionine that is Highly Mutagenic for S. typhimurium
TAlOO. W.R. Leopold, J.A. Miller, and E.C. Miller. Biochem.
Biophys. Res. Commun. 88:395-401, 1979.
- Carcinogenicity
of Antitumor cis-Platinum(II) Coordination Complexes in the
Mouse and Rat. W.R. Leopold, E.C. Miller, and J.A. Miller.
Cancer Res. 39:913-918, 1979.
- Mutagenicity,
Tumorigenicity, and Electrophilic Reactivity of the Stereoisomeric
Platinum(II) Complexes of 1,2-Diaminocyclohexane. W.R. Leopold,
R.P. Batzinger, J.A. Miller, E.C. Miller, and R.H. Earhart.
Cancer Res. 41:4368-4377, 1981.
- Toxicity
and Anticancer Activity of a New Triazine Antifolate (NSC 127755).
T.H. Corbett, W.R. Leopold, D.J. Dykes, B.J. Roberts, D.P.
Griswold, Jr., and F.M. Schabel, Jr. Cancer Research 42:1707-1715,
1982.
- Comparison
of some Carcinogenic, Mutagenic, and Biochemical Properties
of S-vinylhomocysteine and Ethionine. W.R. Leopold, J.A. Miller,
and E.C. Miller. Cancer Res. 42:4364-4374, 1982.
- Induction
and Chemotherapeutic Response of Two Transplantable Ductal
Adenocarcinomas of the Pancreas in C57BL/6 Mice. T.H. Corbett,
B.J. Roberts, W.R. Leopold, J.C. Peckham, L.J. Wilkoff, D.P.
Griswold, Jr., and F.M. Schabel, Jr. Cancer Res. 44:717-726,
1984.
- Biochemical
Pharmacology of the Lipophilic Antifolate, Trimetrexate, R.C.
Jackson, D.W. Fry, T.J. Boritzki, J.A. Besserer, W.R. Leopold,
B.J. Sloan, and E.F. Elslager. Adv. Enzyme. Reg. 22:187-206,
1984.
- 5-[(Aminoalkyl)amino]-Substituted
Anthra[1,9-cd]pyrazol-6(2H)- ones as Novel Anticancer Agents.
Synthesis and Biological Evaluation. H.D.H. Showalter, J.L.
Johnson, L.M. Werbel, W.R. Leopold, R.C. Jackson, and E.F.
Elslager. J. Med. Chem. 27:253-255, 1984.
- Anticancer
Activity of the Structurally Novel Antibiotic, CI-920, and
its Analogs. W.R. Leopold, J. L. Shillis, A.E. Mertus, J.M.
Nelson, B.J. Roberts, and R.C. Jackson. Cancer Res. 44:1928-1932,
1984.
- The
Biochemical Pharmacology of CI-920, a Structurally Novel Antibiotic
with Antileukemic Activity. R.C. Jackson, D.W. Fry, T.J. Boritzki,
B.J. Roberts, K.E. Hook, and W.R. Leopold. Adv. Enzyme Regulation.
23:193-215, 1985.
- Biochemical
and Antitumor Activity of Tiazofurin and its Selenium Analog
(2-˜-D-ribofuranosyl-4-selenazolecarboxamide ). T.J. Boritzki,
D.A. Berry, J.A. Besserer, P.D. Cook, D.W. Fry, W.R. Leopold,
and R.C. Jackson. Biochem. Pharmacol. 34:1109-1114, 1985.
- Collagen
Production Inhibitors Evaluated as Antitumor Agents. W.D. Klohs,
R.D. Steinkampf, M.S. Wicha, A.E. Mertus, J.B. Tunac, and W.R.
Leopold. JNCI, 75:353-359, 1985.
- Dezaguanine
Mesylate: A New Antipurine Antimetabolite. W.R. Leopold, D.W.
Fry, T.J. Boritzki, J.A. Besserer, I.C. Pattison, and R.C.
Jackson. Invest. New Drugs, 3:223-231, 1985.
- The
Anthrapyrazoles, A New Class of Intercalating Agents with High
Level, Broad Spectrum Activity Against Murine Tumors. W.R.
Leopold, J.M. Nelson, J. Plowman, and R.C. Jackson. Cancer
Res. 45:5532-5539, 1985.
- Biochemical
Pharmacology and Experimental Chemotherapy Studies With The
Anthrapyrazole CI-937, a Synthetic Intercalating Agent With
Broad-Spectrum Murine Anticancer Activity. R.C. Jackson, D.W.
Fry, W.R. Leopold, J.S. Sebolt, W.D. Klohs, H.D.H. Showalter,
L.M. Werbel, and E.F. Elslager. Recent Adv. Chemother. J. Ishigamic
(ed). U. Tokyo Press, Tokyo, pp. 568-569, 1985.
- Cell
Cycle Effects of Trimetrexate (CI-898). K.E. Hook, J.M. Nelson,
B.J. Roberts, D.P. Griswold, Jr., and W.R. Leopold. Cancer
Chemother.
& Pharmacol. 16:116-120, 1986.
- Biological
and Biochemical Activities of the Novel Antitumor Antibiotic
PD 114,759 and Related Derivatives. D.W. Fry, J.L. Shillis,
and W.R. Leopold. Inv. New Drugs, 4:3-10, 1986.
- In
Vivo and In Vitro Anticancer Activity of the Structurally Novel
and Highly Potent Antibiotics CI-940 and its Hydroxy Analog
PD 114721. B.J. Roberts, K.L. Hamelehle, J.S. Sebolt, and W.R.
Leopold. Cancer Chemother. & Pharmacol. 16:95-101, 1986.
- The
Biochemical Pharmacology of (2'-R)-Chloropentostatin, A Novel
Inhibitor of Adenosine Deaminase. R.C. Jackson, W.R. Leopold,
and D.A. Ross. Adv. Enzyme Regulation. 25:125-139, 1986.
- Pyrazole
Derivatives. V. Synthesis and Antineoplastic Activity of 3-(2-Chloroethyl)-3,4-dihydro-4-oxopyrazolo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide
and Related Compounds. C.C. Cheng, E.F. Elslager, L.M. Werbel,
S. Priebe, and W.R. Leopold. J. Med. Chem. 29:1544-1547, 1986.
- Design,
Biochemical Pharmacology, Electrochemistry, and Tumor Biology
of Antitumor Anthrapyrazoles. H.D.H. Showalter, D.W. Fry, W.R.
Leopold, J.W. Lown, J.A. Plambeck, and K. Reszka. Anticancer
Drug Design 1:73-85, 1986.
- In
Vivo and In Vitro Evaluation of 5-[4-substituted aryl)-1-piperazinyl]-6-alkyl-2,4-pyrmidinediamines
as Antitumor Agents. L.M. Werbel, J. Hung, J.A. Besserer, T.J.
Boritzki, W.R. Leopold, and D.W. Fry. IN: Chemistry and Biology
of Pteridines 1986, B.A. Cooper, and V.M. Whitehead (eds),
Walter de Gruyter & Co., Berlin, pp. 69-71, 1986.
- Curative
Chemotherapy of Advanced and Disseminated Solid Tumors of Mice.
T.H. Corbett, B.J. Roberts, A.J. Lawson, and W.R. Leopold.
IN: Head and Neck Cancer: Scientific Perspectives in Management
and Strategies for Cure. Jacobs, J.R., Al-Serraf, M., Crissman,
J., and Valeriote, F. (eds.), Elsevier Scientific Publishing
Co., Inc., New York, pp. 175-192, 1987.
- Therapeutic
Synergy of Trimetrexate (CI-898) in Combination with Doxorubicin,
Vincristine, Cytoxan, 6-Thioguanine, Cisplatin, or 5-Fluorouracil
Against Intraperitoneally Implanted P388 Leukemia. W.R. Leopold,
D.J. Dykes, and D.P. Griswold, Jr. NCI Mono. (5):99-104, 1987.
- 5-Aminoanthrapyrazoles
(CI-937, CI-941, CI-942): A Novel Class of DNA Binders with
Broad Spectrum Anticancer Activity. In New Avenues in Developmental
Cancer Chemotherapy (Vol. 8 of Bristol-Myers Cancer Symposium
Series). L.M. Werbel, E.F. Elslager, D.W. Fry, R.C. Jackson,
W.R. Leopold, and H.D.H. Showalter. Harrap, K.R. and Connors,
T.A. (eds.), Academic Press, Orlando, FL, pp. 355-365, 1987.
- Biological
Effects of Acetomycin. I. Activity Against Tumor Cells In Vitro
and In Vivo. S.W. Mamber, J.D. Mitulski, K.A. Hamelehle, J.C.
French, G.C. Hokanson, J.L. Shillis, W.R. Leopold, D.D. Von
Hoff, and J.B. Tunac. J. Antibiotics. 40(1):73-76, 1987.
- Biochemical
Pharmacology and Experimental Chemotherapy Studies with Guanine-7-oxide,
a Novel Purine Antibiotic. R.C. Jackson, T.J. Boritzski, J.A.
Besserer, W.R. Leopold, and D.W. Fry. Adv. Eng. Reg. 26:301-316,
1987.
- Anthrapyrazole
Anticancer Agents. Synthesis and Structure- Activity Relationships
Against Murine Leukemias. H.D.H. Showalter, J.L. Johnson, J.M.
Hoftiezer, W.R. Turner, L.M. Werbel, W.R. Leopold, J.L. Shillis,
R.C. Jackson and E.F. Elslager. J. Med. Chem. 30(1):121-131,
1987.
- Experimental
Antitumor Activity of the Amacrine Analogue CI-921. W.R. Leopold,
T.H. Corbett, D.P. Griswold, Jr., J. Plowman, B.C. Baguley.
JNCI 79:343-349, 1987.
- Benzothiopyranoindazoles,
A New Class of Chromophore Modified Anthracenedione Anticancer
Agents. Synthesis and Activity Against Murine Leukemias. H.D.H.
Showalter, M.M. Angelo, E.M. Berman, G.D. Kanter, D.F. Ortwine,
S.G. Ross-Kesten, A.D. Sercel, W.R. Turner, L.M. Werbel, D.F.
Worth, E.F. Elslager, W.R. Leopold, and J.L. Shillis. J. Med.
Chem. 31:1527-1539, 1988.
- Preclinical
Studies With Trimetrexate: A Review of Conclusions and Unanswered
Questions. R.C. Jackson, W.R. Leopold, K.L. Hamelehle, and
D.W. Fry. Sem. Oncology, 15:1-7, 1988.
- Design,
Tumor Biology, and Biochemical Pharmacology of Anthrapyrazoles.
H.D.H. Showalter, L.M. Werbel, W.R. Leopold, D.W. Fry, W.D.
Klohs, and R.C. Jackson. In: Anthracycline and Anthracenedione-based
Anticancer Agents, J.W. Lown (ed), Elsevier, Amsterdam, pp.
201-243, 1988.
- Activity
of the Pyrazoloacridines Against Multidrug Resistant Tumor
Cells. J.S. Sebolt, M.J. Havlick, K.L. Hamelehle, J.M. Nelson,
W.R. Leopold, and R.C. Jackson. Cancer Chemother. Pharmacol.
24:219-224, 1989.
- Sequence
and Schedule Dependent Synergy of Trimetrexate in Combination
with 5-Fluorouracil in vitro and in mice. W.L. Elliott, C.T.
Howard, D.J. Dykes, and W.R. Leopold. Cancer Res. 49(20):49:5586-5590,
1989.
- Biochemical
Pharmacology and Antitumor Properties of 4-amino-8-[˜-D-ribofuranosylamino]pyrimido-[5,4,-d]
pyrimidine. R.C. Jackson, T.J. Boritzki, P.D. Cook, K.E. Hook,
W.R. Leopold, and D.W. Fry. Adv. Enz. Reg. 28:185-199, 1989.
- The
Pyrazoloacridines: Approaches to the Development of a Carcinoma-Selective
Cytotoxic Agent. R.C. Jackson, J.S. Sebolt, J.L. Shillis, and
W.R. Leopold. Cancer Investigation, 8:39-47, 1990.
- Antitumor
Activity of Ethyl 5-Amino-1,2-dihydro-2-methyl-3-phenyl-pyrido[3,4,-b]pyrazin-7-ylcarbamate,
2-Hydroxyethanesulfonate, Hydrate (NSC 370147) Against Selected
Tumor Systems in Culture and in Mice. W.R. Waud, W.R. Leopold,
W.L. Elliott, D.J. Dykes, W.R. Laster, C.G. Temple, S.D. Harrison,
Jr., and D.P. Griswold, Jr. Cancer Res. 50:3239-3244, 1990.
- Antitumor
Efficacy of PD 115934 (NSC 366140) Against Solid Tumors of
Mice. P. LoRusso, A.J. Wozniak, L. Polin, D. Capps, W.R. Leopold,
L.M. Werbel, L. Biernat, M.E. Dan, and T.H. Corbett. Cancer
Res. 50:4900-4905, 1990.
- Preclinical
Antitumor Activity of CI-973, [SP-4-3-(R)]-[1,1-cyclobutanedicarboxylato(2-)](2-methyl-1,4-butanediamine-N,N')
platinum. A.J. Kraker, C.W. Moore, B.J. Roberts, W.R. Leopold,
W.L. Elliott. Investigational New Drugs, 9(1):1-7, 1991.
- In
Vivo and In Vitro Evaluation of the Alkylating Agent Carmethazole.
W.L. Elliott, D.W. Fry, W.K. Anderson, J.M. Nelson, K.E. Hook,
P.A. Hawkins, and W.R. Leopold. Cancer Res. 51:4581-4587, 1991.
- A
New Class of Analogs of the Bifunctional Radiosensitizer ˜-(1-Aziridinylmethyl)-2-nitro-1H-imidazole-1-ethanol
(RSU 1069): The Cycolalkylazindines. M.J. Suto, M.A. Stier,
L.M. Werbel, C.M. Arundel-Suto, W.R. Leopold, and J.S. Sebolt-Leopold.
J. Med. Chem. 2 34:2484-2488, 1991.
- Pharmacologic/Pharmacokinetic
Evaluation of Emesis Induced by Analogs of RSU1069 and its
Control by Antiemetic Agents. J.S. Sebolt-Leopold, P. Vincent,
K. Beningo, W. Elliott, W. Leopold, M. Stier, and M. Suto.
Int. J. Radiation Oncol. Biol. and Phys. 22(3):549-551, 1992.
- Dual
Function Nitroimidazoles Less Toxic than RSU1069: Selection
of Candidate Drugs for Clinical Trial (RB6145 and/or PD 130908).
S. Cole, I.J. Stratford, E.M. Fielden, G.E. Adams, W. Leopold,
W. Elliott, M. Suto, and J. Sebolt-Leopold. Int. J. Rad. Oncol.
Biol. and Phys. 22(3):545-548, 1992.
- Chemical
Approaches To Improved Radiotherapy. W.R. Leopold and J.S.
Sebolt-Leopold. Proceedings of the 22nd Annual Cancer Symposium
on Anticancer Drug Discovery and Development. F.A. Valeriote,
T.H. Corbett, L.H. Baker (eds). Kluwer Academic Press, pp.
179-196, 1992.
- Comparative
Molecular Field Analysis of In Vitro Growth Inhibition of L1210
and HCT-8 Cells by Some Pyrazoloacridines. J.P. Horwitz, I.
Massova, T.E. Wiese, T.H. Corbett, J.S. Sebolt-Leopold, D.B.
Capps, and W.R. Leopold. J. Med. Chem. 36:3511-3516, 1993.
- Inhibition
of 5-phosphoribosyl-1-pyrophosphate (PRPP) Synthase by the
Monophosphate Metabolite of 4-amino-8-(˜-D-ribrofuranosylamino)
pyrimido-[5,4-d]Pyrimidine: A Novel Mechanism for Antitumor
Activity. D.W. Fry, T.J. Boritzki, R.C. Jackson, D.P. Cook,
and W.R. Leopold. Molecular Pharm. 44(2):479-485, 1993.
- Chemotherapy
with [SP-4-3-(R)]-[1,1-Cyclobutanedicarboxylato(2-)](2-methyl-1,4-butanediamine-N,N')platinum(CI-973,
NK121) in Combination with Standard Agents against Murine Tumors
in Vivo. W.L. Elliott, B.J. Roberts, C.T. Howard, W.R.Leopold
III. Cancer Research, 54:4412-4418, 1994.
- A
Specific Inhibitor of the Epidermal Growth Factor Receptor
Tyrosine Kinase, D.W. Fry, A.J. Kraker, A. McMichael, L.A.
Ambroso, J.M. Nelson, W.R. Leopold, R.W. Connors, A.J. Bridges.
Science 265:1093-1095, 1994.
- Pharmaceutical
Issues Important to the Development of PD 144872 (CI-1010),
the R-Isomer of RB 6145. J.S. Sebolt-Leopold, M.J. Suto, W.L.
Elliott, H.D.H. Showalter, and W.R. Leopold. Documentation
of the MRC Conference on Successful Exploitation of Biomedical
Research, IBC, March 7-8, 1994.
- Strategies
for the Discovery of Novel Tyrosine Kinase Inhibitors with
Anticancer Activity. D.W. Fry, A.J. Kraker, R.C. Connors, W.L.
Elliott, J.M. Nelson, H.D. Showalter and W.R. Leopold. Anti-Cancer
Drug Design, 9:331-351, 1994.
- Tumor
Models and the Discovery and Secondary Evaluation of Solid
Tumor Active Agents. T. Corbett, F. Valeriote, P. LoRusso,
L. Polin, C. Panchapor, S. Pugh, K. White, J. Knight, L. Demchik,
J. Jones, L. Jones, N. Lowichik, L. Biernat, B. Foster, A.
Wozniak, L. Lisow, M. Valdivieso, L. Baker, W. Leopold, J.
Sebolt, M. Bissery, M. Mattes, J. Dzubow, J. Rake, R. Perni,
M. Wentland, S. Coughlin, J.M. Shaw, G. Liversidge, E. Liversidge,
J. Bruno, R. Moore and G. Patterson. International Journal
of Pharmacognosy, 33 (Supplement): 102-122, 1995.
- Inhibition
of the epidermal growth factor receptor tyrosine kinase by
PD 153035 in human A431 tumors in athymic nude mice. Kunkel,
M.W., Hook, K.E., Howard, C.T., Przybranowski, S.A., Roberts,
B.J., Elliott, W.L. and Leopold, W.R. Investigational New Drugs
13:295-302, 1996.
- Cellular
Transport of CI-980. Hook, K.E., Przybranowski, S.A. and Leopold,
W.R. Investigational New Drugs 14:341-347, 1996.
- Treatment
of Human Prostate Tumor LNCaP with Standard and Investigational
Agents in SCID Mice. L. Polin, J. Jones, L. Demchik, P. LoRusso,
C. Panchapor, S. Pugh, K. White, J. Knight, L. Jones, L. Biernat,
D. Visscher, L. Lisow, K.C. Mattes, P. Sarpotdar, E. Liversidge,
G. Liversidge, J. Bruno, M. Shaw, J. Rake, W. Leopold, III,
R.E. Moore, G. Patterson, F. Valeriote, L. Baker and T.H. Corbett.
The Prostate.
- Amino-terminal
Sequence Determinants for Substrate Recognition by Platelet-Derived
Growth Factor Receptor Tyrosine Kinase. P.M. Chan, P.R. Keller,
R.W. Connors, W.R. Leopold, W.T. Miller. FEBS-Lett.121-125,
1996
- Preclinical
Anti-tumor Activity of CI-994 (Acetyldinaline, PD 123654),
LoRusso PM, Demchik L., Foster B, Knight J., Bissery MC, Polin
LM, Leopold WR, Corbett TH. Investigational New Drugs 14:349-356,
1996.
- Enhanced
Therapeutic Effect of Amsalog (CI-921) in Combination with
Cisplatin in vitro and in vivo. Elliott, W.L., Howard, C.T.,
Roberts, B.J., Hook, K.E., Vincent, P.W., Corbett, T.H., and
Leopold, W.R. Oncology Reports 3:1153-1159, 1996.
- Chemotherapy
with DMXAA (5,6-dimethylxanthenone-4-acetic acid) in combination
with CI-1010 (1H-imidazole-1-ethanol, alpha-[[(2-bromoethyl)amino]methyl]-2-nitro-,mono-hydrobromide
(R isomer) against advanced stage murine colon carcinoma 26.
Vincent PW, Roberts BJ, Elliott WL, and Leopold WR. Oncology
Reports Vol. 4:143-147, 1997.
- C-Terminal
Modifications of Histidyl-(N-Benzylglycinamides) to Give Improved
Inhibition of Ras Farnesyltransferase, Cellular Activity and
Anticancer Activity in Mice. McNamara, D.L., Dobrusin, E.,
Leonard, D.M., Shuler, K.R., Kaltenbronn, J.S., Quin, J., Bur,
S., Thomas, C.E., Doherty, A.M., Scholten, J.D., Zimmerman,
K.K., Gibbs, B.S., Gowan, R.C., Latash, M.P., Leopold, W.R.,
Przybranowski, S.A., Sebolt-Leopold, J.S., J. Med. Chem. 40(21):3319-3322,
1997.
- Specific,
irreversible inactivation of the epidermal growth factor receptor
and erbB2, by a new class of tyrosine kinase inhibitors. Fry
DW, Bridges AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook
KE, Keller PR, Leopold WR, Loo JA, McNamara DJ, Nelson JM,
Sherwood V, Smaills JB, Trumpp-Kallmeyer S, Dobrusin EM. Proc.
Natl. Acad. Sci. USA. 95:12022-12027, 1998.
- Regulation
of metastasis-related gene expression by p53: A potential clinical
implication. Sun, Y., Wicha, M., Leopold, WR. Molecular Carcinogenesis
24:25-28, 1999.
- Growth
inhibition of nasopharyngeal carcinaoma cells by EGF receptor
tyrosine kinase inhibitors. Sun, Y., Fry, D.W., Vincent, P.,
Nelson, J., Elliott, W., Leopold, W.R. Anticancer Res. 19(2A):919-924,
1999.
- Tyrosine
kinase inhibitors. 15.4-(phenylamino) quinazoline and 4-(phenylamino)
pyrido{d}pyrimidine acrylamides as irreversible inhibitors
of the ATP binding site of the epidermal growth factor receptor.
Smaill JB, Palmer BD, Rewcastle GW, Denny WA, McNamara DJ,
Dobrusin EM, Bridges AJ, Zhou H., Showalter H, Winters RT,
Leopold WR, Fry DW, Nelson JM, Slintak V, Elliott WL, Roberts
BJ, Vincent PW, Patmore SJ. Journal of Medicinal Chemistry.
42:1803-1815, 1999.
- Blockade
of the MAP kinase pathway suppresses growth of colon tumors
in vivo. Sebolt-Leopold JS, Dudley DT, Herrera R, Van Becelaere
K, Wiland A, Gowa RC, Tecle H, Barrett SD, Bridges A, Przybranowski
S, Leopold WR, Saltiel AR. Nature Medicine. 5:810-816, 1999.
- Anticancer
efficacy of the irreversible EGFr tyrosine kinase inhibitor
PD 0169414 against human tumor xenografts. PW Vincent, AJ Bridges,
DJ Dykes, DW Fry, WR Leopold, SJ Patmore, BJ Roberts, S Rose,
V Sherwood, H. Zhou, WL Elliott. Cancer Chemother. & Pharmacol.
45:231-238, 2000.
- Pyrido[2,3-d]pyrimidin-7-one
Inhibitors of Cyclin-Dependent Kinases. M Barvian, DH Boschelli,
J Cossrow, E Dobrusin, A Fattaey, A Fritsch, D Fry, P Harvey,
P Keller, M Garrett, F La, W Leopold, D McNamara, M Quin, S
Trumpp-Kallmeyer, P Toogood, Z Wu, E Zhang. J. Med. Chem. 43,
4606-4616, 2000.
- 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines
and related 2-urea derivatives are potent and selective inhibitors
of the FGF receptor-1 tyrosine kinase. AM Thompson, CJ Connolly,
JM Hamby, S Boushelle, BG Hartl, AM Amar, AJ Kraker, DL Driscoll,
RW Steinkampf, SJ Patmore, PW Vincent, BJ Roberts, WL Elliott,
W Klohs, WR Leopold, HD Showalter, WA Denny. Journal of Medicinal
Chemistry. 43(22):4200-11, 2000.
- Cell
Cycle and Biochemical Effects of PD 0183812; A Potent Inhibitor
of Cyclin-D Dependent Kinases CDK4 and CDK6. DW Fry, PH Harvey,
D Bedford, A Fritsch, PR Keller, Z Wu, E Dobrusin, WR Leopold,
A Fattaey, MD Garrett. J. Biol. Chem. 276(20):16617-16623,
2001.
- Differential
utilization and localization of ErbB receptor tyrosine kinases
in skin compared to normal and malignant keratinocytes. Stoll
SW, Kansra S, Peshick S, Fry DW, Leopold WR, Wiesen JF, Sibilia
M, Zhang T, Werb Z, Derynck R, Wagner EF, Elder JT. Neoplasia
(New York). 3(4):339-350, 2001.
- Radiosensitization
of p53 mutant cells by PD 0166285, a novel G(2) checkpoint
abrogator. Y Wang, J Li, RN Booher, A Kraker, T Lawrence, WR
Leopold, Y Sun. Cancer Research. 61(22):8211-8217, 2001.
- Transplantable
Syngeneic Rodent Tumors: Solid Tumors of Mice. In Tumor Models
in Cancer Research (Teicher, BA ed). TH Corbett, BJ Roberts,
AJ Lawson, WR Leopold, K White, J Kushner, J Paluch, S Hazeldine,
R Moore, J Rake, and JP Horowitz. Humana Press, Totowa, NJ.
Chapter 2, 41-71, 2002.
- Growth
Factor and Signal Transduction Targets for Cancer Therapy.
Anticancer Drug Development (B.C. Baguley and D.J. Kerr, eds.)
WR Leopold, A Bridges, S Decker, DW Fry, A Kraker, J Sebolt-Leopold.
Academic Press, San Diego: Chapter 3:pp 31-53, 2002.
- Radiosensitization
by pan erbB Inhibitor CI-1033 in Vitro and in Vivo. MK Nyati,
D Maheshwari, S Hanasoge, A Sreekumar, SD Rynkiewicz, AM Chunnaiyan,
WR Leopold, SP Ethier, TS Lawrence. Clin. Cancer. Res. 10:691-700,
2004.
- The
influence of tumor size and environment on gene expression
in commonly used human tumor lines. M Gieseg, M Man, N Gorski,
S Madore, E Kaldjian, WR Leopold. Biomed Central 4:35, 2004.
- Specific
inhibition of cyclin-dependent kinase 4/6 by PD0332991 and
associated antitumor activity in human tumor xenografts. DW
Fry, PJ Harvey, PR Keller, WL Elliott, M Meade, E Trachet,
M Albassam, X Zheng, WR Leopold, NK Pryer, and PL Toogood.
Molecular Cancer Therapeutics 3(11), 1427-1437, 2004.
- Plasma
vascular endothelial growth factor and interleukin-8 as biomarkers
of antitumor efficacy of a prototypical erbB family tyrosine
kinase inhibitor. JG Christensen, PW Vincent, WD Klohs, DW
Fry, WR Leopold, WL Elliott. Molecular Cancer Therapeutics
4(6), 938-947, 2005.
- Real-Time imaging of emerging drug resistance during cancer therapy. KC Lee, DE Hall, BA Hoff, BA Moffat, S Sharma, TL Chenevert, CR Meyer, WR Leopold, TD Johnson, A Rehemtulla, and BD Ross. Cancer Research 66(9) 4687-4692, 2006.
- Dynamic imaging of emerging resistance during cancer therapy. KC Lee, DE Hall, BA Hoff, BA Moffat, S Sharma, TL Chenevert, CR Meyer, WR Leopold, TD Johnson, RV Mazurchuk, A Rehemtulla, and BD Ross. Cancer Research, 66(9) 4687-4692, 2006.
- Magnetic resonance imaging determination of tumor grade and early response to temozolomide in a genetically engineered mouse model of glioma. P McConville, D Hambardzumyan, JB Moody, WR Leopold, AR Kreger, MJ Woolliscroft, A Rehemtulla, BD Ross, and EC Holland. Clinical Cancer Research, 13(10) 2897-2904, 2007.
- Preclinical models of tumor growth and response. P McConville, WL Elliott, A Kreger, R Lister, JB Moody, E Trachet, F Urban, and WR Leopold. In In Vivo Imaging of Cancer Therapy (AF Shields and P Price, eds) Humana Press, New Jersy, Chapter 2, pp 13-32, 2007.
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Invited Presentations : |
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- Therapeutic Synergy of Trimetrexate (CI-898) in Combination with Doxorubicin, Vincristine, Cytoxan, 6-Thioguanine, Cisplatin, or 5-Fluorouracil Against Intraperitoneally Implanted P388 Leukemia. At the Symposium on "Development of Folates and Folic Acid Antagonists in Cancer Chemotherapy." Tarpon Springs, Florida. January 23-26, 1986.
- The Use of In Vivo Murine Tumor Systems for Selection of Lead Compounds. At the Approaches to Antineoplastic Drug Discovery Symposium/Phase 1 - BMAG Meeting. November 17, 1986.
- Strategies for the Discovery and Development of DNA Binding Agents with Improved Spectra of Anticancer Activities. Meeting of the Southwestern Oncology Group, October 12, 1989.
- Chemical Approaches to Improved Radiotherapy. At the Twenty-Second Annual Detroit Cancer Symposium of Wayne State University School of Medicine, Detroit, Michigan. April 26-28, 1990.
- Preclinical Evaluation of the Anticancer Activity of Pentostatin. At the 15th International Cancer Congress. Hamburg, F.R. Germany, August 16 22, 1990.
- In vivo evaluation of signaling antagonists-Potential pitfalls and opportunities. At the AACR/EORTC/BACR meeting on "Cell Signaling and Cancer Treatment." San Juan, Puerto Rico, December 5 9, 1993.
- Search for Signaling Antagonists with Anticancer Activity. Grand Rounds, H. Lee Moffitt Cancer Center and Research Institute, U. South Florida. May 6, 1994.
- Therapeutic Potential and Discovery of Signaling Antagonists with Anticancer Activity. Inaugural Lecture in the "Target Selection and Drug Design" lecture series. Purdue University Cancer Center, Experimental Therapeutics Program. July 1, 1994.
- Small Molecule Inhibitors of ras Related Signal Transduction Pathways and Problems Associated with their Evaluation. Banbury Conference on Neurofibromatosis. Cold Spring Harbor Laboratory. October 16-18, 1995.
- Potent, Highly Selective and Irreversible Inhibitors of the EGF Receptor Family of Tyrosine Kinases: Long Held Dogma of Pharmacology Put to the Test. Leopold, WR. NATO Advanced Research Workshop on Protein – Protein and Protein-Lipid Interactions in Signal Transduction: Use of Small Synthetic Molecules as Probes and Therapeutic Agents. Clearwater Beach, Florida. December 5-9, 1997.
- Inhibitors of Type I Tyrosine Kinases as Anticancer Agents. New Developments in Cancer Conference (SRI). Princeton, NJ. March 16 17, 1998.
- New Paradigms for Cancer Drug Discovery and their Implications for pre-IND Toxicology. Twentieth Annual Meeting of the American College of Toxicology, McLean, VA. November 7-10, 1999.
- N-Alkoxy-2- (4-iodo-phenylamino)-benzamides: O-Alkyl Benzhydroxamate Esters as a Novel Class of Potent, Selective and Long Acting In Vitro MEK Inhibitors. S.D. Barrett, AJ Bridges, DT Dudley, AR Saltiel, JH Fergus, A Delaney, WR Leopold, SA Przybranowski, J Sebolt-Leopold, K. VanBecelaere, AM Doherty, RM Kennedy, D Marston, WA Howard Jr., H Tecle. Amer. Chem. Soc. Natl. Meeting, 218th. Abstracts of Papers, Pt.1, Abstr. 203. 1999.
- Pharmacodynamically Driven Drug Discovery: Application to the Discovery and Development of MEK Inhibitors. Van Andel Research Institute, Grand Rapids, MI. October 4, 2002.
- MEK Inhibitors as Anticancer Agents: An Example of Pharmcokinetically Guided Drug Discovery and Development. University of New Mexico Cancer Research and Treatment Center Clinical Research Meeting. Albuquerque, NM. January 30, 2003.
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Abstracts : |
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- S-Vinylhomocysteine (Vinthionine): A Highly Mutagenic Analog of Ethionine. W.R. Leopold, J.A. Miller, and E.C. Miller. Proc. Amer. Assoc. Cancer Res. 20:28, 1979.
- Mutagenic and Carcinogenic Properties of Electrophilic Antitumor Dichlorodiammine and 1,2-Diaminocyclohexane Platinum (II) Complexes. W.R. Leopold, R.P. Batzinger, J.A. Miller, E.C. Miller, and R.H. Earhart. Proc. Amer. Assoc. Cancer Res. 22:108, 1981.
- Radiation + Chemotherapy + Surgical Treatment of Solid Tumors of Mice. T.H. Corbett, A.J. Lawson, W.R. Leopold, D.P. Griswold, Jr., F.M. Schabel, Jr., and J.R. Durant. Proc. Am. Assoc. Cancer Res. 23:191, 1982.
- Evaluation of Antitumor Agents Against a Transplantable Mouse Pancreatic Ductal Carcinoma (Panc 02). T.H. Corbett, W.R. Leopold, D.P. Griswold, Jr., F.M. Schabel, Jr. Proc. 13th International Cancer Congress, p. 17, 1982.
- Evaluation of the Acute Toxicity of Combinations of Adriamycin and Aclacinomycin A with Radiation. A.J. Lawson, T.H. Corbett, and W.R. Leopold. Radiat. Res. 91:347, 1982.
- In Vivo Activity of the Novel Anticancer Agent PD 110,161. W.R. Leopold, M.E. Dombrowski, J.M. Nelson, and B.J. Roberts. Proc. Am. Assoc. Cancer Res. 24:320, 1983.
- A Rapidly Growing, High Growth Fraction, Metastatic, Pancreatic Ductal Carcinoma Unresponsive to All Commonly Used Anticancer Agents. T.H. Corbett, W.R. Leopold, S.A. Sapareto, D.P. Griswold, Jr., and F.M. Schabel, Jr. Proc. Am. Assoc. Cancer Res. 24:283, 1983.
- Substituted Anthra[1,9-_c_d] pyrazole-6(2_H) ones. A Novel Family of DNA-Binding Agents with Broad Spectrum Anticancer Activity. W.R. Leopold, J.M. Nelson, B.J. Roberts, A.E. Mertus, C.T. Howard, and T.H. Corbett. Proc. Amer. Assoc. Cancer Res. 25:352, 1984.
- Biological Evaluation of CI-921, A Second-Generation Analog of Amsacrine. W.R. Leopold, J.L. Shillis, T.H. Corbett, and R.C. Jackson. Proc. Am. Assoc. Cancer Res. 25:294, 1984.
- Evaluation of Basement Membrane Collagen as a Target for Chemotherapeutic Intervention. W.D. Klohs, R.W. Steinkampf, M.S. Wicha, A.E. Mertus, and W.R. Leopold. Cell Biology, 99:402a, 1984.
- In Vivo Evaluation of A New Soluble Formulation of Dezaguanine (CI-908) as A Single Agent and In Combination With Clinically Active Anticancer Agents. W.R. Leopold, and R.J. DeLap. Proc. Am. Assoc. Cancer Res. 26:323, 1985.
- In Vivo Activity and Biochemical Characterization of Substituted [1]Benzothiopyrano[4,3,2-cd]indazoles, A Novel Class of DNA-binding Anticancer Agents. W.R. Leopold and D.W. Fry, J.M. Nelson, and J.D. Plowman. Proc. Amer. Assoc. Cancer Res. 26:253, 1985.
- Characterization of a Murine Leukemia Cell Line Selected for In Vivo Resistance to CI-920 (Phosphotrienin). C. Howard, W.R. Leopold, J.S. Sebolt, and R.C. Jackson. Proc. Am. Assoc. Cancer Res. 26:339, 1985.
- Activity of the Highly Potent Novel Anticancer Antibiotic CI 940 (PD 114,720) and its Hydroxy Analog (PD 114,721). B.J. Roberts, J.A. Nelson, J.S. Sebolt, C.T. Howard, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 26:253, 1985.
- 1986.
- Broad Spectrum Antitumor Activity and Biochemical Pharma¬cology of the Novel Anthrapyrazole, CI-941. D.W. Fry, R.C. Jackson, H.D.H. Showalter, L.M. Werbel, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 26:219, 1985.
- Characterization and Drug Sensitivity of an Adriamycin Resistant Subline of B16/BL6 Murine Melanoma In Vitro and In Vivo. M.J. Havlick, J.S. Sebolt, W.R. Leopold, and R.C. Jackson. J. Cell Biol. 101(pt 2):482a, 1985.
- Biochemical Pharmacology and Experimental Chemotherapy Studies with the Anthrapyrazole, CI-937, A Synthetic Inter¬calating Agent With Broad-Spectrum Murine Anticancer Activity. R.C. Jackson, D.W. Fry, W.R. Leopold, J.S. Sebolt, W.D. Klohs, H.D.H. Showalter, L.M. Werbel, and E.F. Elslager. 14th Int. Congress of Chemotherapy (abstracts), 323, 1985.
- Antitumor Activity of a Novel 1,2-Dihydropyrido[3,4-_b] pyrazine in Preclinical Drug-Sensitive and -Resistant Tumors. D.P. Griswold, Jr., C.G. Temple, Jr., M.W. Trader, W.R. Leopold, W.R. Laster Jr., and D.J. Dykes. Proc. Am. Assoc. Cancer Res. 27:306, 1986.
- In Vivo and In Vitro Evaluations of 5-[4-(Substituted Aryl)-1-piperazinyl]-6-alkyl-2,4-pyrimidinediamines as Anti¬tumor Agents. D.W. Fry, L.M. Werbel, J. Hung, J.A. Besserer, T.J. Boritzki, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 27:253, 1986.
- Therapeutic Synergy of Trimetrexate (CI-898) in Combination with Doxorubicin, Cytoxan, 6-Thioguanine, 5-Fluorouracil, Vincristine, or Cisplatin Against P388 Leukemia. W.R. Leopold, D.D. Dykes, and D.P. Griswold, Jr. Proc. Am. Assoc. Cancer Res. 27:253, 1986.
- Biological and Biochemical Properties of the 2-Aminoalkyl-5 nitropyrazolo[3,4,5-_k_l]acridines (Pyrazoloacridines). S.V. Scavone, J.S. Sebolt, C.D. Pinter, M.J. Havlick, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 27:277, 1986.
- Solid Tumor Selectivity of the 2-aminoalkyl-5-nitropyrazolo¬[3,4,5 kl]acridines, A Novel Class of DNA-binding Anti¬tumor Agents. J.S. Sebolt, W.R. Leopold, K.L. Hamelehle, C.D. Pinter, and J.D. Plowman. Proc. Am. Assoc. Cancer Res. 27:421, 1986.
- 5-[4-(Substituted Aryl)-1-piperazinyl]-6-alkyl-2,4-pyrimi¬dine-diamines: A Novel Class of Antifol Antitumor Agents. L.M. Werbel, D.W. Fry, J. Hung, J.A. Besserer, T.J. Boritzki, W.R. Leopold. Int. Symp. Pteridines and Folic Acid Derivatives, June 15-20, 1986.
- Potentiation of Adriamycin, Trimetrexate, and an AMSA Analog (CI-921) Cytotoxicities by Amiodarone and Reserpine in Multidrug Resistant P388 Cells. W.D. Klohs, R.W. Steinkampf, W.R. Leopold, and D.W. Fry. Proc. Am. Assoc. Cancer Res. 28:298, 1987.
- 2-(Aminoalkyl)-5-amino-2H-(1)benzoselenino(4,3,2-cd)-inda¬zoles. A New Class of Selenium Heterocycle with Potent Antitumor Activity. E. Berman, W. Klohs, W.R. Leopold, J. Plowman, A.D. Sercel, J.L. Shillis, H.D.H. Showalter, and L.M. Werbel. Proc. Am. Assoc. Cancer Res. 28:302, 1987.
- Activity and Biochemical Properties of GOE1734 (PD 104208), an Anticancer Agent with a Novel Mechanism of Activity. W.R. Leopold, K.E. Hook, and D.W. Fry. Proc. Am. Assoc. Cancer Res. 28:302, 1987.
- Sequence and Schedule Dependent Synergy of Trimetrexate in Combination with 5-Fluorouracil or Cisplatin. C.T. Howard, K.E. Hook, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 28:417, 1987.
- An In Vitro/In Vivo Solid Tumor Model for Assessing Antitumor Activity Using Murine Melanoma B16 and a Subline Resistant to Adriamycin. M.J. Havelick, K.L. Hamelehle, B.J. Roberts, J.L. Shillis, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 28:451, 1987.
- Anticancer Benzochalcogenoindazoles. Comparative Tumor Biology, Biochemistry, and Aqueous Stability. H.D.H. Showalter, E.M. Berman, J.A. Besserer, D.W. Fry, G.C. Hokanson, W.D. Klohs, W.R. Leopold, L.M. Werbel, and J. Plowman. 194th Am. Chem. Soc. Nat'l. Mtg., New Orleans. MEDI Abstr. 25, 1987.
- Preclinical Characterization of the In Vitro and In Vivo Activity of [1,1] Cyclobutanedicarboxylato(2-)-O,O'] (2-methyl-1,4-butanediamine-N,N')Pt (NK-121/CI-973). A.J. Kraker, C.W. Moore, W.R. Leopold, and K. Takahashi. Proc. Am. Assoc. Cancer Res. 29:344, 1988.
- Correlation Between In Vitro and In Vivo Testing of DNA-binders Versus Antifolates in Multiple-Drug Resistant (MDR) P388 Cells (P388R). W.D. Klohs, J.S. Sebolt, R.W. Steinkampf, M.J. Havlick, E.M. Berman, L.M. Werbel, W.R. Leopold, and R.C. Jackson. Proc. Am. Assoc. Cancer Res. 29:320, 1988.
- Synthesis, Characterization, and Antitumor Properties of Bidentate Aminoalkylcyclo(aza)alkaneplatinum(II) Complexes. J.D. Hoeschele, W.R. Leopold, A.J. Kraker, and D.A. Berry. Proc. Am. Assoc. Cancer Res. 29:345, 1988.
- Biochemical and Experimental Chemotherapy Studies of the Pyrazolo¬acridines. R.C. Jackson, W.R. Leopold, and J.S. Sebolt. Proc. Am. Assoc. Cancer Res. 29:536, 1988.
- A New Class of Analogues of the Bifunctional Radio¬sensi¬tizer RSU 1069: The Cycloalkylaziridines. C.M. Arundel-Suto, W.L. Elliott, W.R. Leopold, L.M. Werbel, M.J. Suto, and J.S. Sebolt. Presented at the 1989 meeting of the Radiation Research Society.
- In Vivo and Biochemical Evaluation of the Novel Alkylator, Carmethizole. W.R. Leopold, D.W. Fry, P. Hawkins, and W.K. Anderson. Proc. Am. Assoc. Cancer Res. 30:469, 1989.
- Development of Resistance to the Anthrapyrazole CI 937 in L1210 Cells. W. Klohs, R. Steinkampf, A. McMichael, J. Nelson, W. Leopold, J. Wolverton, and W. Beck. Proc. Am. Assoc. Cancer Res. 30:523, 1989..
- The Development of a New Class of Bifunctional Radiosensitizers: The Cycloalkylaziridines. J.S. Sebolt, C.M. Arundel-Suto, W.L. Elliott, W.R. Leopold, L.M. Werbel, and M.J. Suto. Proc. Am. Assoc. Cancer Res. 30:551, 1989.
- Analogs of the Bifunctional Radiosensitizer RSU 1069. M.J. Suto, M.A. Stier, J.S. Sebolt, W.R. Leopold, C.M. Arundel-Suto, W.L. Elliott, and L.M. Werbel. Ann. Mtg. Amer. Chem. Soc., Miami, FL. 1989.
- Antitumor Efficacy of PD 115934 (NSC 366140) Against Solid Tumors of Mice. P. LoRusso, A. Wozniak, L. Polin, D. Capps, W. Leopold, L. Werbel, L. Biernat, and T. Corbett. Proc. Am. Assoc. Cancer Res. 31:411, 1990.
- In Vivo Evaluation of a New Potent Inhibitor of ADP-ribosyltransferase Activity, PD 128,763. W.L. Elliott, J.S. Sebolt-Leopold, W.R. Leopold, and D.W. Siemann. Proc. Am. Assoc. Cancer Res. 31:418, 1990.
- In Vitro and In Vivo Evaluation of the Radiosensitizer, PD 130908, an Analog of RSU1069 with Superior Potency and Reduced Toxicity. W.R. Leopold, C.M. Arundel-Suto, W.L. Elliott, P.W. Vincent, and J.S. Sebolt-Leopold. Proc. Am. Assoc. Cancer Res. 31:393, 1990.
- Preclinical Evaluation of PD 130908, a Desoxy Analog of RSU1069 with Superior Potency and Reduced Toxicities. J.S. Sebolt-Leopold, C.M. Arundel-Suto, W.L. Elliott, L.M. Werbel, M.J. Suto, and W.R. Leopold. Presented at the 1990 Meeting of the Radiation Research Society.
- Cardiotoxic Potential of CI-958, A New DNA-Intercalator in Mice. S.N. Kim and W.R. Leopold. Toxicologic Pathology, 18:696, 1990.
- Effects of PD 128763, a New Potent Inhibitor of ADP ribosyltransferase, on Radiation Induced Cellular Recovery Processes in Solid Tumors. D.W. Siemann, J.S. Sebolt Leopold, W.R. Leopold, and W.L. Elliott. Proceedings of the Thirty Eighth Ann. Meeting of the Rad. Res. Society, p. 152, 1990.
- Pharmacologic/Pharmacokinetic Evaluation of Emesis Induced by Analogs of RSU1069 and its Control by Antiemetic Agents. J.S. Sebolt-Leopold, P. Vincent, K. Beningo, W. Elliott, W. Leopold, M. Stier, and M. Suto. 7th Intl. Conf. on Chem. Modifiers of Cancer Treatment. Clearwater, FL. Feb, 1991.
- Dual Function Nitroimidazoles Less Toxic than RSU1069: Selection of Candidate Drugs for Clinical Trial (RB6145 and/or PD 130908). S. Cole, I.J. Stratford, E.M. Fielden, G.E. Adams, W. Leopold, W. Elliott, M. Suto, and J. Sebolt-Leopold. 7th Intl. Conf. on Chem. Modifiers of Cancer Treatment. Clearwater, FL. Feb, 1991.
- A New Class of Bifunctional Nitroimidazole Radiosensitizers Incorporating Soft Alkylating and Acylating Functionality. H.D.H. Showalter, A.D. Sercel, R.T. Winters, W.R. Leopold, W.L. Elliott, C.M. Arundel-Suto, and J.S. Sebolt-Leopold. Proc. Am. Assoc. Cancer Res. 32:389, 1991.
- Combination Chemotherapy with [SP-4-3-(R)]-[1,1-Cyclobutane¬dicarboxylato(2-)](2-methyl-1,4-butanediamine-N,N')platinum (CI-973) and Standard Agents in Murine Tumor Models. W.L. Elliott, B.J. Roberts, K.E. Hook, C.T. Howard, P.W. Vincent, J.M. Nelson, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 32:433, 1991.
- Variations in Growth Characteristics of Murine Neuroblastoma, Neuro-2a, Dependent on Inoculation Route. S.A. Przybranowski, K.E. Hook, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 33:51, 1992.
- Cytotoxicity and Uptake of CI-980 and It's R-Enantiomer, PD 132183. K.E. Hook, S.A. Przybranowski, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 33-427, 1992.
- In Vivo Studies on Multidrug Resistant (MDR) Tumors with the New Chemosensitizer Tioperidone. W.L. Elliott, B.J. Roberts, R.W. Steinkampf, W.R. Leopold, and W.D. Klohs. Proc. Am. Assoc. Cancer Res. 33:478, 1992.
- Synthesis and Biological Evaluation of the Enantiomers of the Radiation Sensitizer RB6145 and Its Cometabolites. A.D. Sercel, V.G. Beylin, O.P. Goel, H.D.H. Showalter, H.J. Betche, W.L. Elliott, W.R. Leopold, and J.S. Sebolt-Leopold. 206th National Meeting, American Chemical Society, Chicago, 1993.
- Studies of the Adduct Formed on Interacting Cisplatin with Human Apotransferrin: Synthesis, In Vitro Binding Kinetics, In Vivo Pharmacokinetics, and Biodistribution in the Rat. J.D. Hoeschele, L.R. Whitfield, W.R. Leopold, W. McNally, J. Nawrocki, and J. Phillips. International Conf. Bioinorganic Chem., San Diego, August 1993.
- In Vivo Evaluation of the Potential for Therapeutic Synergy Between CI 980 and Standard Chemotherapeutic Agents. W.R. Leopold, W.L. Elliott, S.A. Przybranowski, and W.R. Waud. Proc. Am. Assoc. Cancer Res. 34:296, 1993.
- Rationale for Selection of PD 144872, the R Isomer of RB6145 for Clinical Development as a Radiosensitizer. J.S. Sebolt-Leopold, W.L. Elliott, H.D.H. Showalter, and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 34:362, 1993.
- Modulation of the Growth Inhibitory Properties of a Novel Class of Protein Tyrosine Kinase Inhibitors, the 2 thioindoles, by Physiologic Concentrations of Glutathione. W.R. Leopold, S.A. Przybranowski, K.E. Hook, L. Ambroso, and D.W. Fry. Proc. Am. Assoc. Cancer Res. 34:408, 1993.
- Preclinical Antitumor Activity of Acetyldinaline. P.M. LoRusso, L. Demchik, J. Knight, M. Bissery, L. Polin, W.R. Leopold and T.H. Corbett. Proc. Am. Assoc. Cancer Res. 35:401, 1994.
- Epidermal Growth Factor Receptor Tyrosine Kinase in A431 Xenografts: Inhibition by PD 153035 (4-(3-bromoanilino)-6,7-dimethoxyquinazoline). K.E. Hook, M.W. Kunkel, W.L. Elliott, C.T. Howard and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 36:434, 1995.
- Construction, Expression, Purification and Characterization of the EGF Receptor Tyrosine Kinase Catalytic Domain. P.R. Keller, R.W. Connors, A. McMichael, D.W. Fry and W.R. Leopold. Proc. Am. Assoc. Cancer Res. 36:434, 1995.
- In Vivo Activity of the Polyamine Analog Diethynorsperimine (CI-1006) Administered as a Continuous SC Infusion. C.T. Howard, B.J. Roberts, W.L. Elliott, W.R. Leopold and C.W. Porter. Proc. Am. Assoc. Cancer Res. 36:385, 1995.
- Inhibition of ras Farnesyl Protein Transferase by a Series of Substituted Thiosulfuric Acids. R.C. Gowen, D. Ferguson, K. Hook, S. Przybranowski, W.L. Elliott, W.R. Leopold, J. Scholten, G.L. Bolton, J.C. Hodges and J.S. Sebolt-Leopold. Proc. Am. Assoc. Cancer Res. 36:430, 1995.
- Inhibitors of the EGF Receptor Tyrosine Kinase Related to the Picomolar Quinazoline Inhibitor PD 153035. A.J. Bridges, A.M. Thompson, G.W. Rewcastle, W.A. Denny, H. Zhou, D.R. Cody, D.W. Fry, A.J. Kraker, L.A. Ambroso, J.M. Nelson, W.R. Leopold, R.W. Connors, and A. McMichael. Proc. Am. Assoc. Cancer Res. 36:435, 1995.
- Effects of PD 128763, A New Potent Inhibitor of ADP-Ribosyl Transferase on Radiation Induced Cellular Recovery Processes in Solid Tumors, ASTRO Meeting, October 8, 1995.
- Biological Evaluation of Cell Permeable Peptide Inhibitors of ras Inhibitors of ras Farnesyl Transferase. J.S. Sebolt-Leopold, R.C. Gowan, B.S. Gibbs, S. Przybranowski, M. Latash, W.R. Leopold, J. Scholten, K. Zimmerman, D. Hupe, D. Leonard, D. McNamara, S. Bur, G.L. Bolton, A.M. Doherty. Proc. Am. Assoc. Cancer Res. 37: 423 (2886), 1996.
- Cellular Activity of Histidinyl-(N-Benzylglycinamides) Against Ras Farnesyltransferase. JS Sebolt Leopold, RC Gowan, MP Latash, S Przybranowski, WR Leopold, D McNamara, A Doherty, D Leonard. Proc. Am. Assoc. Cancer Res. 38:350, 1997.
- In vivo evaluation of histidine-(N-Benzylglycinamides) as inhibitors of ras farnesyltransferase. SA Przybranowski, WL Elliott, DM Leonard, DJ McNamara, J Quin, KR Shuler, JS Sebolt-Leopold, WR Leopold. Proc. Am. Assoc. Cancer Res. 38:350, 1997.
- Evaluation of the mutational status of ras genes in mouse tumor models used in anticancer drug discovery. R. Merriman, T. Corbett, E. Guisbert, C. Howard, W. Leopold, J. Sebolt-Leopold, B. Young and Y. Sun. Proc. Amer. Assoc. Cancer Res. 38:350, 1997.
- Structure-activity relationships of histidine N-Benzylglycinamides: potent ras farnesyl-transferase inhibitors. DM Leonard, RM Smith, JS Kaltenbronn, KR Shuler, J. Quin, D McNamara, J Scholten, JS Sebolt-Leopold, M Latash, RC Gowan, WR Leopold, S Przybranowski, AM Doherty.
- Influence of fractionated x-irradiation therapy in the assessment of normal tissue response in rats. P Vincent, W Elliott, C Howard, WR Leopold, S Lotarski, R Parker, B Roberts. Proc. Amer. Assoc. Cancer Res. 38:247, 1997.
- Histidinyl-(N-Benzylglycinamides) as ras farnesyltransferase inhibitors possessing antitumor activity in mice. DJ McNamara, EM Dobrusin, DM Leonard, KR Shuler, KM Smith, JS Kaltenbronn, J Quinn III, AM Doherty, S Bur, CE Thomas, JD Scholten, KC Zimmerman, JS Sebolt Leopold, RC Gowan, MP Latash, WR Leopold, SA Przybranowski. American Chemical Society. 1997.
- Decreased invasiveness of ras-transformed tumor cells associated with inhibition of farnesyltransferase. JS Sebolt-Leopold, RC Gowan, D Driscoll, WD Klohs, Y Sun, D. Hupe, T Peterson, D McNamara, D Leonard. Proc. Amer. Assoc. Cancer Res, 1997.
- Inhibition of ras farnesyl transferase by a series of histidine-(benzylglycinamides) with antitumor activity. DM Leonard, JS Kaltenbronn, AM Doherty, KR Shuler, J Quinn III, D McNamara, J Scholten, M Latash, RC Gowan, WR Leopold, S Przybranowski, JS Sebolt-Leopold. American Chemical Society, P. Medi, 1998.
- Design of petidomimetic RAS farnesyl transferase inhibitors from a pentapeptide lead. DM Leonard, KR Shuler, D McNamara, GL Bolton, J Scholten, K Zimmerman, JS Sebolt-Leopold, RC Gowan, M Latash, S Przybranowski, WR Leopold, AM Doherty. Pept, 1996, Proc. Eur. Pept. Symp. 24th 1998.
- Tyrosine Phosphorylation of Human Estrogen Receptor by Stat 1. K Shen, RF Novak, SC Brooks, JS Sebolt-Leopold, WR Leopold. Proc. Amer. Assoc. Cancer Res, 1998.
- Pyrido[2,3-d]pyrimidines as inhibitors of cyclin-dependent kinases. Z Wu, D Boschelli, E Dobrusin, A Fattaey, A Fritsch, MD Garrett, P Keller, WR Leopold, M Quinn, S Trumpp-Kallmeyer, DW Fry. University of Michigan, Cancer Research Symposium, 1998.
- The ineradicable impact of irreversible inhibitors: Can erbBicide contribute to the tumouricide of EGFr-dependent cancers? AJ Bridges, WA Denny, EM Dobrusin, AM Doherty, WL Elliott, DW Fry, K Hook, WR Leopold, DJ McNamara, JW Nelson, BD Palmer, S Patmore, GW Rewcastle, BJ Roberts, HDH Showalter, V Slintak, JB Smaill, AM Thompson, S Trumpp-Kallmeyer, PW Vincent, RT Winters, H Zhou. Proceedings of the XVth International Symposium on Medicinal Chemistry, 1998.
- Application of neural networks in development of structure-pharmacokinetic relationships. J Vora, C Lathia, S Przybranowski, J Hollembaek, J Blankley, D Leonard, J Kaltenbronn, J Sebolt Leopold, R Feng, W Li, WR Leopold. American Association of Pharmaceutical Scientists, San Francisco, CA, 1998.
- SAR and anti-angiogenic activity of a series of FGF selective tyrosine kinase inhibitors. CJC Connolly, JM Hamby, MC Schroeder, MR Barvian, GH Lu, T Dahring, RL Panek, A Amar, C Chen, AJ Kraker, DW Fry, D Driscoll, WD Klohs, HDH Showalter, WR Leopold, AM Doherty, K Brown. American Chemical Society Meeting.
- Characterization of the in vivo activity of a novel EGF receptor family kinase inhibitor, PD 169414. PW Vincent, BE Atkinson, H Zhou, DJ Dykes, WR Leopold, S Patmore, B Roberts, AJ Bridges, WL Elliott. Proc. Amer. Assoc. Cancer Res. 1998.
- In vivo evaluation of in vivo of the irreversible EGF receptor tyrosine kinase inhibitor PD 168393. S Patmore, B Roberts, CL Stoner, PW Vincent, WR Leopold, DJ Dykes, WA Denny, JB Smaill, WL Elliott. Proc. Amer. Assoc. Cancer Res. 1998.
- Development of irreversible EGFr tyrosine kinase inhibitors with anti-tumor activity against human tumor xenografts. JB Smaill, WA Denny, DW Fry, JM Nelson, WR Leopold, PW Vincent, KE Hook, WL Elliott, AJ Bridges, H. Zhou, HDH Showalter, DJ McNamara, DM Dobrusin. NCI-EORTC Conference, Amsterdam Netherlands, 1998.
- Development, structure-activity relationships and anti-tumor activity of a novel class of specific, irreversible EGFR TK inhibitors. JB Smaill, WA Denny, DW Fry, JM Nelson, WR Leopold, PW Vincent, SJ Patmore, WL Elliott, KE Hook, AJ Bridges, H. Zhou, HDH Showalter, DJ McNamara, EM Dobrusin. BACR Conference, Dublin Ireland, 1998.
- Potent and Selective MEK Kinase Inhibitors: Synthesis and SAR of 2-(4-iodo phenylamino)-benzoic acids and hydroxamic acid derivatives thereof.. Tecle H, Barrett S, Bridges A, Leopold J, Dudley D, Przybranowski S, Leopold W, Saltiel A, Doherty A. Proc Am Assoc Cancer Res 40:121 (Abstract 806), March 1999.
- Cell cycle and biological effects of PD 171851, a specific inhibitor of cyclin-dependent kinase 4 (CDK4). JM Nelson, D Boschelli; Z Wu; A Fattaey, MD Garrett, PR Keller, WR Leopold and DW Fry. Keystone Symposia, The Molecular Basis of Cancer. March 15-21, 1999 Taos, NM.
- N-Alkoxy-2-(4-iodo-phenylamino)-benzamides: O-Alkyl Benzhydroxamate Esters as a Novel Class of Potent, Selective and Long Acting In Vitro MEK Inhibitors. S.D. Barrett, AJ Bridges, DT Dudley, AR Saltiel, JH Fergus, A Delaney, WR Leopold, SA Przybranowski, J Sebolt-Leopold, K. VanBecelaere, AM Doherty, RM Kennedy, D Marston, WA Howard Jr., H Tecle. Amer. Chem. Soc. Natl. Meeting, 218th. Abstracts of Papers, Pt.1, Abstr. 203. 1999.
- Potent and selective MEK inhibitors: Synthesis and SAR of 2-(4-iodo-phenylamino) benzoic acids and hydroxamic acid derivatives thereof.. H Tecle, S Barrett, A Bridges, J Leopold, D Dudley, S Przybranowski, W Leopold, A Saltiel, A Doherty. Proc. Amer. Assoc. Cancer Res. 40:121, 1999.Preclinical combination studies of N-acetyl-dinaline (CI-994) with standard anticancer agents in acute myeloid leukemia (AML). CL Vanderwilt, EM Comijn, JM Padron, HF Teshale, WR Leopold, RL Merriman, GJ Peters. Proc. Amer. Assoc. Cancer Res. 41:239, 2000.
- Cell cycle and biochemical effects of PD 0183812, a specific inhibitor of cyclin-dependent kinase 4. DW Fry, PJ Harvey, PR Keller, Z Wu, E Dobrusin, WR Leopold, A Fattaey, M Garrett. Proc. Amer. Assoc. Cancer Res. 41:314, 2000.
- Gene expression profiling of anti-tumor efficacy of the irreversible EGFR/erbB family inhibitor CI-1033 in vivo. JG Christensen, J Messamore, E Ferguson, TA Jatkoe, PW Vincent, WR Leopold, SJ Madore, WL Elliott. Proc. Amer. Assoc. Cancer Res. 41:482, 2000.
- Onyx-015 (CI-1042), a p53-Selectively Replicating Adenovirus, Armed with Prodrug Converting Enzymes. L Cohen, W Collard, C Omer, W Leopold. Abstract from Sixth McGill University International Conference on Eukaryotic DNA Replication. Cold Spring Harbor Laboratory Meeting, Cold Spring Harbor, New York. September 5-9, 2001
- The Ineradicable Impact of Irreversible Inhibitors: can erbBicide contribute to the tumouricide of EGFr-dependent cancers? AJ Bridges, WA Denny, EM Dobrusin, AM Doherty, WL Elliott, DW Fry, K Hook, WR Leopold, DJ McNamara, JM Nelson, BD Palmer, S Patmore, GW Rewcastle, BJ Roberts, HDH Showalter, V Slintak, JB Smaill, AM Thompson, S Trumpp-Kallmeyer, PW Vincent, RT Winters and H Zhou. In Medicinal Chemistry into the Millennium, M. C. Campbell and I. S. Blagbrough eds., Royal Society of Chemistry, Cambridge, England. 2001
- In vivo evaluation of MEK inhibitor, CI-1040 (PD 0184352), against a panel of human pancreatic tumor xenografts. EE Trachet, SA Przybranowski, CT Howard, H Auble, K Van Becelaere, H Valik, CM Loi, JS Sebolt-Leopold, DJ Dykes, SD Barrett, H Tecle, WR Leopold, RL Merriman. Proc. Amer. Assoc. Cancer Res. 5426:2096, 2002.
- Radio-Sensitization by Pan Erbb-2 Inhibitor CI-1033 In Vitro and In Vivo. MK Nyati, A Sreekumar, SD Rynkiewicz, A Chinnaiyan, WR Leopold, SP Ethier and TS Lawrence. Proc. Am. Assoc. Cancer Res. 2002
- The effects of tumor size and mouse strain on tumor xenograft gene expression. Michael A. Gieseg, Michael Z. Man, Nicolas A. Gorski, Steven J. Madore, William L. Elliott and Wilbur R. Leopold III. Oncogenomics 2003, Dissecting cancer through genome research. Jan 29-Feb 2, 2003 Phoenix Arizona. Abstract 2522.
- Diffusion MRI in preclinical drug testing: an early surrogate marker for efficacy in subcutaneous human tumor xenografts. J Moody, P McConville, RJ Lister, AR Kreger, E Trachet, WL Elliott, BA Moffit, TL Chenevert, DL Dexter, A Rehemtulla, BD Ross, WR Leopold. Proc. Am. Assoc. Cancer Res. 2004.
- High field MRI characterization of tumor growth kinetics, vascularity and cellularity in a PDGF-driven RCAS/tv-a mouse model of glioma. PJ McConville, JB Moody, RJ Lister, AR Kreger, E Trachet, WL Elliott, A Rehemtulla, BD Ross, EC Holland, W. R. Leopold. Proc. Am. Assoc. Cancer Res. 2004.
- High-throughput MRI in the use and development of preclinical mouse tumor models. PJ McConville, JB Moody, BD Ross, WR Leopold. Proc. Amer. Assoc. Cancer Res. 2004.
- Synthesis and SAR development of PD03259901, a potent and highly bioavailable MEK inhibitor. Michael D. Kaufman, D. Barett, Cathlin M. Flamme, Yvonne D. Smith, Manoj Cheriyan, Luyan Zhang, Haile Tecle, Judith Sebolt-Leopold, Heather Valik, Richard Gowan, Keri Van Becelaere, Ronald Merriman, Sally Przybranowski, Jeffery Ohren, Christopher Whitehead, W.R. Leopold, Ellen Dobrusin, Alexander Bridges. Proc. Amer. Assoc. Cancer Res. 2004.
- The Biological Profie of PD 0325901: A second generation analog of CI-1040 with improved pharmaceutical potential. Judith S. Sebolt-Leopold, Ronald Merriman, Charles Omer, Haile Tecle, Alex Bridges, Wayne Klohs, Cho-Ming Loi, Heather Valik, Sally Przybranowski, Mark Meyer, W.R. Leopold. Proc. Amer. Assoc. Cancer Res. 2004.
- Highly selective inhibition of Cdk4 with pyridol[2.3-d] pyrimidin-7-ones. Scott N. Vanderwel, Patricia J. Harvey, Derek J. Sheehan, Joseph Repine, Paul R. Keller, John Booth, John Quin III, Dennis J. McMamera, Hairong Zhou, Ellen Dobrusin, Alexander J. Bridges, Wilbur R. Leopold, David W. Fry, Joanne Brodfuehrer, Tong, Zhu, Peter L. Toogood. Amer. Assoc. Cancer Res. 2004.
- Inhibition of Cdk4 causes tumor regression. John Booth, William Elliott, David W. Fry, Patricia Harvey, Paul Keller, W. R. Leopold, Dennis McNamera, Maryanne Meade, Nancy Pryor, Joseph Repine, Derek Sheehan, Peter L. Toogood, Erin Trachet, Scott Vanderwel, Hairong Zhou. Proc. Amer. Assoc. Cancer Res. 2004.
- Characterization of a novel MEK inhibitor (PD181461) which inhibits human hepatocellular carcinoma growth in vitro and in vivo. Earl A. Gage, Chad A. Wiesenauer, Jennifer N. Choi, Patrick J. Klein, Michelle T. Yip Schneider, Yufang Wang, Faith Albertin, Judy S. Sebolt-Leopold, Christian M. Schmidt. Proc. Amer. Assoc. Cancer Res. 2004
- Gene expression changes link to efficacy in human tumor xenografts treated with the CDK4/6 inhibitor PD0332991. Seth Sadis, Xianxian Zheng, Mary Anne Meade, Clarence Lewis, Mark Molloy, Laura Fleischer, Steven J. Madore, Li Xi, Megan Robinson, Eric Kaldjian, William Elliott, Wilber R. Leopold, David W. Fry. Proc. Amer. Assoc. Cancer Res. 2004.
- PK/PD modeling of biomarker (p-ERK) response and tumor growth to PD 0325901 in a human tumor xenograft mouse model. Jeffrey R. Koup, Jing Liu, Cho-Ming Loi, Curtis Howard, Keri Van Becelaere, Sally Przybranowski, Justin Walton, Judith Sebolt-Leopold, Ronald Merriman. Proc. Amer. Assoc. Cancer Res. 2004.
- Survivin protein expression is markedly reduced in human colon cancer xenografts treated with the CDK4/6 inhibitor PD 3329991. Eric P. Kaldjian, Mark J. Cameron, Seth Sadis, Mary Anne Meade, W.R. Leopold, William Elliott, David W. Fry. Proc.Amer. Assoc. Cancer Res. 2004.
- Diffusion MRI in preclinical drug testing: An early surrogate marker for efficacy in subcutaneous human tumor xenografts. Jonathan B. Moody, Patrick McConville, Richard J. Lister, Alicia R. Kreger, Erin Trachet, William L. Elliott, Bradford A. Moffat, Thomas L. Chenevert, Daniel L. Dexter, Alnawaz Rehemtulla, Brian D. Ross, W. R. Leopold. Proc. Am. Assoc. Cancer Res. 44: 5116, 2004.
- High field MRI characterization of tumor growth kinetics, vascularity and cellularity in a PDGF-driven RCAS/tv-a mouse model of glioma. Patrick J. McConville, Jonathan B. Moody, Richard J. Lister, Alicia R. Kreger, Erin Trachet, William L. Elliott, Alnawaz Rehemtulla, Brian D. Ross, Eric C. Holland, W. R. Leopold. Proc. Am. Assoc. Cancer Res. 44: 5115, 2004.
- High-throughput MRI in the use and development of preclinical mouse tumor models. Patrick J. McConville, Jonathan B. Moody, Brian D. Ross, W. R. Leopold. Proc. Amer. Assoc. Cancer Res. 44: 213, 2004.
- MRI determination of temozolomide treatment response in a tv-a transgenic model of glioma. Patrick J. McConville, Jonathan B. Moody, Alicia R. Kreger, Erin Trachet, Richard J. Lister, William L. Elliott, W. R. Leopold, Eric C. Holland. Proc. Amer. Assoc. Cancer Res. 2005;46:3787.
- MRI predicts tumor grade and survival in a tv-a transgenic model of glioma. Jonathan B. Moody, Alicia R. Kreger, Patrick J. McConville, Erin Trachet, Richard J. Lister, William L. Elliott, W. R. Leopold, Eric C. Holland. Proc. Amer. Assoc. Cancer Res. 2005;46:1068.
- In vivo imaging of a mouse model of PC-3 bone metastasis. Jonathan B. Moody, Richard J. Lister, Patrick J. McConville, Alnawaz Rehemtulla, William L. Elliott, W. R. Leopold. Proc. Amer. Assoc. Cancer Res. 2005;46:3796.
- In vivo micro-CT of mouse lungs without respiratory gating. Erin Trachet, Jonathan B. Moody, Patrick J. McConville, William L. Elliott, W. R. Leopold. Proc. Amer. Assoc. Cancer Res. 2005;46:3795.
- Evaluation of MRI in a mouse model of liver metastasis. Alicia R. Kreger, Patrick J. McConville, William L. Elliott, W. R. Leopold. Proc. Amer. Assoc. Cancer Res. 2005;46:3794.
- Bioluminescence imaging of apoptosis correlates with diffusion MRI detection of cell kill after treatment of subcutaneous D54 xenografts. Patrick J McConville, Jonathan B Moody, Alicia R Kreger, William L Elliott, Wilbur R Leopold, Brian D Ross, Alnawaz Rehemtulla. Proc. Amer. Assoc. Cancer Res. 2006:47:2389.
- Preclinical efficacy prediction using diffusion MRI. Jonathan B Moody, Patrick J McConville, Richard J Lister, Bradford A Moffatt, Thomas L Chenevert, Alnawaz Rehemtulla, Brian D Ross, Wilbur R Leopold. Proc. Amer. Assoc. Cancer Res. 2006:47:2388.
- Intratumoral injection of BCNU in ethanol (DTI015) and BCNU in ethanol/PEG400 cure subcutaneous C26 tumors. Richard J Lister, Patrick McConville, William L Elliott, Wilbur R Leopold, Brian D Ross, Alnawaz Rehemtulla, John M Young, Edward E Luck. Proc. Amer. Assoc. Cancer Res. 2006:47:5448.
- Efficacy of temozolomide in a transgenic model of glioma: MRI determined tumor growth inhibition and diffusion response are predictive of survival. Patrick J McConville, Jonathan B Moody, Richard J Lister, William L Elliott, Wilbur R Leopold, Eric C Holland. Proc. Amer. Assoc. Cancer Res. 2006:47:2756.
- Diffusion MRI early prediction of survival using solvent facilitated perfusion of BCNU in a rat model of glioma. Patrick McConville, Jonathan B Moody, Richard J Lister, William L lliott, Wilbur R Leopold, Brian D Ross, Alnawaz Rehemtulla, John M Young, Edward E Luck. Proc. Amer. Assoc. Cancer Res. 2006:47:2746.
- Synergistic activity of aflibercept (VEGF Trap) in combination with 5-fluorouracil and irinotecan in preclinical tumor models. MF Chiron, P Vrignaud, P Lejeune, B Demers, WR Leopold, MC Bissery. Proc. AACR-EORTC Int. Conf. Molecular Targets and Cancer Therapeutics. 2007:69, A13.
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