AACR ACS 
CHEMISTRY IN CANCER RESEARCH:
A Vital Partnership in Cancer Drug Discovery and Development

A joint conference presented by the American Association for Cancer Research and the American Chemical Society

February 8-11, 2009 • Westin New Orleans Canal Place • New Orleans, LA
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Conference Chairperson:
John T. Hunt, Bristol-Myers Squibb, Princeton, NJ

Scientific Program Committee:
Matthew A. Marx, Pfizer, San Diego, CA
Brent R. Stockwell, Columbia University, New York, NY
David A. Wink, National Cancer Institute, Bethesda, MD
Cheryl L. Zimmerman, University of Minnesota College of Pharmacy, Minneapolis, MN

* - Short talk from proffered paper

February 8  
6:30-8:00 p.m.  Keynote Lectures
 

Introduction of Dr. Larry J. Marnett
John T. Hunt, Bristol-Myers Squibb, Princeton, NJ

Cyclooxygenase Inhibitors in Cancer Detection, Prevention, and Treatment
Larry J. Marnett, Vanderbilt University, Nashville, TN

Introduction of Dr. Gregory L. Verdine
Brent R. Stockwell, Columbia University, New York, NY

Interrogation, Recognition, and Repair of Damaged Bases in DNA
Gregory L. Verdine, Harvard University, Cambridge, MA

8:00 – 9:00 p.m.    Welcome Dessert Reception
February 9
7:00 – 8:00 a.m.   Continental Breakfast
8:00 – 9:45 a.m.    Session 1:  Chemistry in Support of Cancer Target ID and Validation

Session Chair: Brent R. Stockwell, Columbia University, New York, NY

Probing Cell Death with Small Molecules
Brent R. Stockwell

Multi-dimensional Chemical Genetics in Cancer
Alexis Borisy, CombinatoRx, Inc., Cambridge, MA

Title to be announced
Benjamin F. Cravatt, Scripps, La Jolla, CA

*Disrupting the Rb-Raf-1 Protein-protein Interaction: A New Strategy for Anticancer Drug Design 
Nicholas J. Lawrence, Moffitt Cancer Center and Research Institute, Tampa, FL

9:45-10:15 a.m. Coffee Break
10:15 a.m.-12:00 p.m. Session 2:  Chemistry in Support of Lead Discovery/Chemical Libraries

Session Chair: Michael Foley, Broad Institute, Cambridge, MA

Natural Product-based Libraries for Chemical Biology and Drug Discovery
Derek S. Tan, Memorial Sloan-Kettering Cancer Center

Build-couple-pair Strategy for Diversity-oriented Synthesis Yields Small Molecule that Binds Hedgehog and Blocks Its Signaling in Human Cells
Michael Foley

Achieving Synthetic Control When Nature Abandon Selectivity
Scott A. Snyder, Columbia University, New York, NY

* Establishment of Novel Antitumor Drugs Screening Method by Using Chemical Array
Siro Simizu, RIKEN, Wako, Saitama, Japan

12:00 – 1:30 p.m.  Lunch on own or Professional Advancement Session
1:30 – 3:15 p.m. Session 3:  Chemistry in Support of Lead Discovery/Screening, Hit Validation, and Natural Products

Session Chairperson: Steven E. Hall, Lync Pharma, Research Triangle Park, NC 

Self-Selecting Drug Discovery: Nucleotide Affinity Resin-Based Screening for Simultaneous Hit and Target Identification
Steven E. Hall

Beyond Natural Products: Function Oriented Synthesis and New Leads for Cancer and Overcoming Cancer Resistance
Paul A. Wender, Stanford University, Stanford, CA

Concise Synthetic Analogs of FR901464: Anti-tumor Compounds Targeting the Spliceosome 
Thomas R. Webb, St. Jude Children's Research Hospital, Memphis, TN

* Carteriosulfonic Acids A-C: Inhibitors of GSK3-β Identified From a Wnt Signaling Assay 
Malcolm W. McCulloch, University of Utah, Salt Lake City, UT

3:15 – 3:45 p.m. Coffee Break
3:45 – 5:30 p.m.  Session 4:  Chemistry in Support of Lead Discovery/Chemoinformatics
Session Chairperson: Patrick Zarrinkar, Ambit Biosciences, San Diego, CA

High Throughput Kinase Profiling: A New Approach to Lead Discovery
Patrick Zarrinkar

A Systems Approach to Therapeutic Discovery
John Westwick, Odyssey Thera, San Ramon, CA

In silico Discovery of Small Molecules Targeting Transcription Factors in Cancer and Inflammation
Alan C. Rigby, Harvard Medical School, Boston, MA

 *3D QSAR Analysis of Pyrazole Derivatives and the Design of Novel Benzimidazole Derivatives 
Leyte L. Winfield, Spelman College, Atlanta, GA

5:30 – 7:30 p.m.  Poster Session A and Cocktail Reception
February 10
7:00 – 8:00 a.m. Continental Breakfast
8:00 – 9:45 a.m. Session 5:  Chemistry in Support of Lead Optimization/Case Histories I

Session Chair: Matthew A. Marx, Pfizer, San Diego, CA

The Discovery of BMS-641988:  A Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer
Aaron Balog, Bristol-Myers Squibb, Princeton, NJ

GDC-0449: A Small Molecule Antagonist of the Hedgehog Pathway
James C. Marsters, Jr., Genentech, Inc., South San Francisco, CA

Discovery of Eltrombopag, a Small-Molecule, Oral Thrombopoietin Receptor Agonist: From Screening to the Clinic
Juan I. Luengo, GlaxoSmithKline, Collegeville, PA

*Synthesis and Anti-Tumor Properties of Pyrazolopyrimidines: Potent, ATP Competitive, and Selective Inhibitors of the Mammalian Target of Rapamycin (mTOR) 
 David J. Richard, Wyeth Discovery Medicinal Chemistry, Pearl River, NY

9:45-10:15 a.m. Coffee Break 
10:15 a.m.-12:00 p.m. Session 6: Chemistry in Support of Cancer Drug Discovery/Case Histories II
Session Chairperson: Danzhou Yang, University of Arizona, Tucson, AZ

DNA G-quadruplexes as Potential Anticancer Drug Targets
Danzhou Yang

The Discovery and Development of Diaryl-acylsulfonamide (Tasisulam Sodium, ASAP): A Novel Class of Antitumor Agents for Solid Tumors
Chuan Joe Shih, Eli Lilly Research Laboratories, Indianapolis, IN

From HTS to Clinic: Discovery of PF-4217903 as Potent and Exquisitely Selective c-Met Inhibitor
Jean Cui, Pfizer Global R & D, San Diego, CA

* DNA Ligase Inhibitors Identified by Computer Aided Drug Design as Novel Cancer Therapeutics 
Xi Chen, University of Maryland, Baltimore, MD

12:00 - 2:00 p.m. Poster Session B and Light Lunch
2:00 – 3:45 p.m. Session 7:  Chemistry in Support of Cancer Drug Targeting, Drug Delivery, and Drug Disposition I
Session Chairperson: Frederick W. Goldberg, AstraZeneca, Inc., Macclesfield, United Kingdom

Antibody-Drug Conjugates for Cancer Therapy
Peter D. Senter, Seattle Genetics, Inc., Bothel, WA

Chemical Modifications for Making Drugs out of RNA Interference
Kallanthottathil G. Rajeev, Alnylam, Cambridge, MA

Use of Phosphate Prodrugs to Improve Solubility: Development of AZD1152, a Soluble and Selective Aurora B Kinase Inhibitor
Frederick W. Goldberg

*New Chemical Probes for Site-Directed Targets Generated by Focused Ultrasound 
Daniel Lee, The Methodist Hospital Research Institute, Houston, TX

3:45 – 4:15 p.m. Coffee Break
4:15 – 6:00 pm. Session 8:  Chemistry in Support of Cancer Drug Targeting, Drug Delivery, and Drug Disposition II
Session Chairperson: Cheryl L. Zimmerman, University of Minnesota, Minneapolis, MN

Multifunctional Nanotherapeutics for Cancer Treatment
Tamara Minko, Rutgers University, New Brunswick, NJ

Surface-functionalization of Nanoparticles for Multi-targeted Drug Delivery 
Jayanth Panyam, University of Minnesota, Minneapolis, MN

Folate Targeted Therapies for Cancer
Christopher P. Leamon, Endocyte, West Lafayette, IN

*Protein-passivated Fe3O4 Nanoparticles: Low Toxicity and Rapid Heating for Thermal Therapy 
Haoheng Yan, University of Massachusetts, Amherst, MA

February 11
7:00 – 8:00 a.m. Continental Breakfast
8:00 – 9:45 a.m. Session 9:  Chemistry in Support of Cancer Drug Discovery and Development I
Session Chairperson: David A. Wink, Jr., National Cancer Institute, Bethesda, MD

Molecular Imaging Studies in Cancer
Murali Krishna, National Cancer Institute, Bethesda, MD

Role of Hyperpolarized 13C Spectroscopic Imaging in Drug Development
John Kurhanewicz, University of California, San Francisco, San Francisco, CA

Measuring Spatial and Temporal Molecular Changes in Tissues Using Imaging Mass Spectrometry
Richard M. Caprioli, Vanderbilt University, Nashville, TN

*Semi-Synthesis of a Hydrocarbon-Stabilized Transcription Factor, Max 
Eileen J. Kennedy, Harvard University, Cambridge, MA

9:45 – 10:15 a.m. Coffee Break
10:15 a.m. - 12:00 p.m. Session 10: Chemistry in Support of Cancer Drug Discovery and Development II

Session Chairperson: John T. Hunt, Bristol-Myers Squibb, Princeton, NJ

ABT-869: Process Development on a VEGF Inhibitor for the Treatment of Cancer
Albert Kruger, Abbott Laboratories, North Chicago, IL                                         

Microheterogeneity and Analytical Approaches to Macromolecules
Randal B. Bass, Amgen, Inc., Seattle, WA

Systems and Controls for Handling Potent Anticancer Agents
Rebecca Ahn, Ash Stevens, Inc., Detroit, MI

*V-PROLI/NO: A Liver Selective Nitric Oxide Prodrug
Sam Hong, National Cancer Institute, Frederick, MD

Departure