2012 National Medicinal Chemistry
Symposium
CONFERENCE CO-HOSTS
Dr. Danzhou Yang
Associate
Professor
Departments of
Pharmacology/Toxicology and Chemistry/Biochemistry
Dr. Chris Hulme
Professor
Departments of
Pharmacology/Toxicology and Chemistry/Biochemistry
PROGRAM COMMITTEE
Dr. Marcel Patek, Sanofi Aventis
Dr. Robin Polt,
Department of Chemistry and Biochemistry
Dr. Leslie
Gunatilaka, Natural Products Center
Dr. Georg
Wondrak, Department of Pharmacology and Toxicology
Dr. Victor
Hruby, Honorary Co-Chair, Department of Chemistry and Biochemistry
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Symposium Registration: May 20th, 2012 8:00 – 18:00 Convention Corridor Welcome
Reception: 19:45 Patio |
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Day 1 Sunday, May 20th |
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9:00
– 18:00 |
Day
1 May 20th, 2012 Symposium Registration Convention Corridor |
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9:00-12:00 |
Graduate
Student and Postdoctoral Scholar Career Development Workshop |
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9:00 – 9:45 |
Alex Dömling (University of Groningen) |
ANCHOR.QUERY APPROACH TO LEVERAGE THE VERY LARGE
CHEMICAL SPACE OF MULTICOMPONENT REACTIONS |
A1 |
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9:45-10:30 |
Antonia
Stepan (Pfizer
Global Research and Development ) |
THE IMPACT OF OXETANE AND [1.1.1]-BICYCLOPENTANE
MOTIFS ON BIOPHARMACEUTICAL PROPERTIES AS APPLIED TO THE
DESIGN OF POTENT AND ORALLY ACTIVE Γ-SECRETASE INHIBITORS |
A2 |
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10:30-11:10 |
Nag Kumar (Simon Fraser University) |
OPTIMIZATION AND STRUCTURE ACTIVITY RELATIONSHIPS
OF A SERIES OF POTENT INHIBITORS OF METHACILLIN RESISTANT STAPHYLOCOCCUS
AUREUS (MRSA) PYRUVATE KINASE AS NOVEL ANTIMICROBIAL AGENTS |
A3 |
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11:15-11:45 |
COFFEE BREAK |
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12:45- 13:00 |
Welcome
from Dr. Jay Gandolfi University
of Arizona |
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13:00-13:15 |
OPENING REMARKS Drs. Danzhou Yang and Chris Hulme University
of Arizona |
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13:15 |
Oral Session 1.
Natural Product Based Drug Discovery and Design Chair: Leslie Gunatilaka,
University of Arizona |
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13:20 |
Ralph Mazitschek
(Harvard) |
Chemogenomic approaches
to novel antimalarials
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1 |
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14:00 |
Brian Blagg (Kansas University) |
USING NATURAL PRODUCT HSP90 INHIBITORS AS A
SOURCE FOR LEAD OPTIMIZATION |
2 |
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14:40 |
Jon Njardarson (University of Arizona) |
Natural Products and New
Synthetic Methods as Entry Points to Medicinal Chemistry
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3 |
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15:20 |
Luke Whitesell
(Whitehead Institute, MIT) |
USING YEAST AS A HIGH THROUGHPUT PLATFORM FOR
DRUG DISCOVERY ACROSS DIVERSE HUMAN DISEASES |
4 |
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16:00 |
Leslie Gunatilaka (University of Arizona) |
STRUCTURE-ANTICANCER ACTIVITY RELATIONSHIPS OF
WITHAFERIN A ANALOGUES |
5 |
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16:40 |
COFFEE BREAK |
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16:55 |
Oral Session 2.
Enabling Technologies in Medicinal Chemistry Chair: Stevan Djuric, Abbott |
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17:00 |
Stevan Djuric (Abbott) |
THE UTILITY OF ENABLING
CHEMISTRY TECHNOLOGY FOR THE REDUCTION OF DRUG DISCOVERY CYCLE TIME |
6 |
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17:40 |
Nick Terrett (Ensemble Therapeutics Corp) |
MOVING IN NEW CIRCLES – EXPLOITING
MACROCYCLES FOR DRUG DISCOVERY (DNA PROGRAMMED CHEMISTRY) |
7 |
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18:20 |
Lyn Jones (Pfizer) |
USING
CHEMICAL PROTEOMICS TO UNDERSTAND DRUG-PROTEIN INTERACTIONS
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8 |
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19:00 |
Werngard Czechtizky (Sanofi Aventis) |
Accelerating
innovation in medicinal chemistry |
9 |
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19:45 |
WELCOME
RECEPTION |
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6:30-8:00 |
Day
2 Monday, May 21st Breakfast |
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8:00 |
Oral Session 3.
Targeting Neurodegeneration Chair: Stephen Hitchcock, Envoy therapeutics |
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8:05 |
Andrew Stamford (Merck Research Laboratories) |
Discovery of Orally
Active, Brain Penetrant BACE Inhibitors: Potential Disease Modifying Agents
for the Treatment of Alzheimer's Disease
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10 |
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8:45 |
Harrie Gijsen (Janssen Research & Development) |
Gamma-Secretase
Modulators for the treatment of Alzheimer’s Disease:
Can we combine potency with safety?
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11 |
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9:25 |
Brian C. Shook (Johnson & Johnson PRD) |
Optimization of Dual
Adenosine A2A/A1 Antagonists for Parkinson’s Disease
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12 |
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10:05 |
COFFEE BREAK |
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10:20 |
Oral
Session 4. Allosteric Modulators (GPCRs/Kinases) Chair: Victor Hruby, University of Arizona |
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10:25 |
Nicholas Cosford
(Sanford|Burnham Medical Research Institute, La Jolla) |
GROUP II METABOTROPIC GLUTAMATE RECEPTORS (MGLURS): DESIGN,
SYNTHESIS AND CHARACTERIZATION OF ALLOSTERIC MODULATORS
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13 |
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11:05 |
Hugh Rosen
(The Scripps
Research Institute, La Jolla) |
S1P1 receptor-ligand interactions at 2.8A
resolution
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14 |
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11:45 |
Douglas Beshore (Merck) |
Pyrazolo[4,3-c]quinolin-3-one-Derived Selective M1 Receptor Positive Allosteric
Modulators
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15 |
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12:25 |
LUNCH SEMINAR IUPAC-Richter Prize in Medicinal Chemistry presented by István Greiner Stephen Hanessian (University of Montreal) DESIGN AND SYNTHESIS OF DRUG PROTOTYPES INSPIRED BY
NATURAL PRODUCTS |
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14:35 |
Oral Session 5. Medicinal Chemistry from the Molecular
Libraries Initiative CHAIR: JEFF AUBE, UNIVERSITY OF
KANSAS |
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14:40 |
Jeff Aube (University
of Kansas) |
Chemical Probe
Development at the University of Kansas
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16 |
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15:20 |
Greg Roth (Sanford–Burnham Medical Research Institute) |
Discovery &
Optimization of Potent & Selective Inhibitors of NOD1 Induced NF-kB
Activation
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17 |
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16:00 |
William Roush
(Scripps–Florida) |
Development of
Proof-of-Concept Chemical Probes Targeting Novel Biological Targets
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18 |
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16:40 |
Craig Thomas (NIH Chemical
Genomics Center) |
Innovations in
Discovery and Translational Research at the NIH Chemical Genomics Center
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19 |
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17:20 |
Michael Foley (Broad Institute) |
Role of
Next-Generation Synthesis in Small-Molecule Probe and Drug Discovery
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20 |
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18:00 |
POSTER SESSION AND RECEPTION |
PS |
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6:30-8:00 |
Day
3 Tuesday, May 22nd Breakfast |
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8:00 |
Oral Session 6. Chromatin Structure and Transcription Chair: David Levens, National Cancer Institute |
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8:05 |
David
Levens (NCI) |
COMPLEX REGULATION OF THE C-MYC
PROMOTER; A PROBLEM OR AN OPPORTUNITY FOR DRUG TARGETING? |
21 |
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8:45 |
Jun
Liu (Johns
Hopkins) |
INHIBITION OF EUKARYOTIC
TRANSCRIPTION BY NATURAL PRODUCTS |
22 |
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9:25 |
James
Bradner (Dana
Farber) |
CHEMICAL
INHIBITION OF BROMODOMAINS IN CANCER THERAPY |
23 |
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10:05 |
Laurence
Hurley (University
of Arizona) |
DRUG
TARGETING OF G-QUADRUPLEXES AND I-MOTIFS IN PROMOTER ELEMENTS |
24 |
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10:45 |
Coffee Break |
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11:00 |
Oral Session 7.
Targeting Autoimmune/Inflammatory Disease Chair: Raj
Singh, Rigel |
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11:05 |
Mike Visnick (Reata) |
Bardoxolone: A phase 3 compound |
25 |
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11:55 |
Jeffrey
Whitten (CalciMedica) |
ORALLY-AVAILABLE CRAC CHANNEL INHIBITORS FOR
TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES |
26 |
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12:35 |
Stefan Tasler (4SC DISCOVERY GmbH) |
EFFICACY IN ANIMAL MODELS OF SMALL MOLECULE
INHIBITORS OF IL-17 SECRETION AND Kv1.3 |
27 |
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13:30 |
TRAVEL TO SABINO CANYON |
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13:30-17:00 |
SABINO
CANYON TRIP WITH
BOXED LUNCH |
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6:30-8:00 |
Day
4 Wednesday, May 23rd Breakfast |
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8:00 |
Oral Session 8.
Anti-infectives and their Inhibitors Chair: Dan Marquess, Theravance |
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8:05 |
Adam Renslo (UCSF) |
Ferrous Iron
Dependent Drug Delivery: More Selective Drug Targeting for Infectious and
Proliferative Diseases?
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28 |
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8:45 |
Richard Elliott (Gates Foundation) |
DRUG DISCOVERY IN NEGLECTED
DISEASES: CHALLENGES AND OPPORTUNITIES |
29 |
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9:25 |
Xiao-Yi (Charlie) Xiao (Tetraphase
Pharmaceuticals) |
DISCOVERY
OF 7-FLUORO-9-PYRROLIDINOACETAMIDO-6-DEMETHYL-6-DEOXYTETRACYCLINE: A POTENT,
BROAD SPECTRUM ANTIBACTERIAL AGENT |
30 |
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10:05 |
Coffee Break |
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10:25 |
James Aggen
(Achaogen) |
BUILDING
UPON WHAT NATURE PROVIDES: THE SEMI-SYNTHETIC ANTIBACTERIAL COMPOUND
PLAZOMICIN |
31 |
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11:05 |
Vincent Hernandez (Anacor) |
THE
DISCOVERY OF GSK2251052: A FIRST-IN-CLASS BORON-CONTAINING ANTIBACTERIAL
AGENT TARGETING LEUCYL TRNA SYNTHETASE |
32 |
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11:45-13:30 |
Lunch |
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13:30 |
Oral Session 9.
Medicinal Chemistry Award Lectures Chair: Jeff Zablocki 2012
Medicinal Chemistry Division Program Chair |
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13:40 |
Suvit
Thaisrivong (Pfizer) Small-Molecule Clinical Candidates Targeting
Autoimmune and Inflammatory Diseases |
33 |
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14:20 |
Steve Fesik (Vanderbilt) |
34 |
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15:00 |
Tomi Sawyer (AILERON Therapeutics) MOLECULAR ARMAMENTARIUM OF CHEMICAL AND
BIOLOGICAL MEDICINES FOR THE WAR ON DISEASE |
35 |
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15:40 |
ACS 2012 Division of Medicinal Chemistry Award Alex Makriyannis (Northeastern University) Traveling the Endocannabinoid Road: New Biology; New
Medications |
36 |
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16:20 |
Closing Remarks |
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18:00 |
Banquet |
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