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Combinatorial Chemistry

Gordon Research Conference

High Throughput Chemistry and Chemical Biology

August 31 - September 5, 2008
Chair Paul R. Hanson
Vice Chair Joseph M. Salvino

Conference Description

This conference is primarily focused on the development of high throughput chemistry and the related biology for accelerating discovery. Topics involving design, production, and use of chemical libraries for addressing targets and pathways of interest to scientists engaged in biomedical, synthetic organic, and/or materials science research are strongly encouraged. Other topics addressed include, advances in technology platforms, informatics, and development of new chemical-biology methods related to libraries. The unifying theme of these topics is the simultaneous exploration of multiple variables at the chemical/biology interface.

Conference Program

SUNDAY
4:00 pm - 9:00 pmArrival and Check-in
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pm High Throughput Technologies
Discussion Leader: Ian Baxendale (Cambridge)
7:40 pm - 8:00 pm Wei Zhang (University of Massachusetts-Boston)
"Fluorous Technologies for Library synthesis"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm Thierry Masquelin / Alex Godfrey (Eli Lilly)
"Integration of an Automated Synthesis Lab in Drug Discovery"
8:40 pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Daryl Sauer (Abbott Laboratories)
"Expanding the Discovery Toolbox with Automation, Inventory Management and Informatics"
9:20 pm - 9:30 pm Discussion
MONDAY
8:00 am - 9:00 amBreakfast
9:00 am - 12:30 pm Molecular Libraries: Hit to Lead
Discussion Leader: Joyce Huang (Pharmacopeia)
9:00 am - 9:25 am Elizabeth Amin (University of Minnesota)
"Novel Hit-to-Lead Strategies Toward Small-Molecule, Druglike Anthrax Toxin Lethal Factor (LF) Inhibitors"/td>
9:25 am - 9:35 am Discussion
9:35 am - 10:00 am John Quinn (AMRI)
"Small Molecule Heterocycle Libraries for Drug Discovery"
10:00 am - 10:10 am Discussion
10:10 am - 10:40 am Coffee Break / Group Photo
10:40 am - 11:05 am Rejean Fortin (Merck Frosst Canada & Co.)
"Exploring Flow Chemistry at Merck Frosst"
11:05 am - 11:15 am Discussion
11:15 am - 11:40 am Benoit DePrez (Institute Pasteur de Lille)
"Protein-templated combinatorial chemistry :a powerful tool to explore ligand binding pockets"
11:40 am - 11:50 am Discussion
11:50 am - 12:20 pm Stefan Bräse (Universität Karlsruhe (TH))
"Diversity-oriented Synthesis of Small Molecular Entities"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session I
6:00 pmDinner
7:30 pm - 9:30 pm Molecular Libraries, Natural Products and Probes
Discussion Leader: Stefan Bräse (Universität Karlsruhe (TH))
7:30 pm - 8:00 pm Derek Tan (Memorial Sloan-Kettering Cancer Center)
"Natural Product-based Strategies in Diversity-Oriented Synthesis"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm Nicolas Winssinger (I.S.I.S. & Université Louis Pasteur)
"Diversity Oriented Synthesis of Natural Products"
8:40pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Scott Gilbertson (University of Texas Medical Branch at Galveston)
"Pilot Libraries Based in Medicinally Relevant Scaffolds"
9:20 pm - 9:30 pm Discussion
TUESDAY
8:00 am - 9:00 amBreakfast
9:00 am - 12:30 pm High Throughput Technologies
Discussion Leader: Tamas Szommer (AMRI)
9:00 am - 9:20 am Matt Clark (GlaxoSmithKline MDR-Boston)
"Synthesis and Screening of DNA-Encoded Small Molecule Libraries"
9:20 am - 9:30 am Discussion
9:30 am - 10:05 am Anthony Barrett (Imperial College London)
"Resorcylates"
10:05 am - 10:15 am Discussion
10:15 am - 10:30 am Coffee Break
10:30 am - 10:55 am Paul Watts (The University of Hull)
"Optimized high throughput chemical synthesis using flow reactors"
10:55 am - 11:05 am Discussion
11:05 am - 11:35 am Mike Organ (York University, Toronto)
"High throughput microfluidic synthesis: from milligrams of many compounds to kilograms of one"
11:35 am - 11:45 am Discussion
11:45 am - 12:20 pm Oliver Kappe (Karl-Franzens-University Graz)
"The magic of microwave chemistry - is it more than rapid heating?"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session II
6:00 pmDinner
7:30 pm - 9:30 pm Chemical Methodologies and Library Development
Discussion Leader: Paul Floreancig (University of Pittsburgh)
7:30 pm - 7:55 pm Scott Schaus (Boston University)
"Asymmetric Boronate Reactions: Condensations, Rearrangements, and Catalysis"
7:55 pm - 8:05 pm Discussion
8:05 pm - 8:35 pm Kay Brummond (University of Pittsburgh)
"Exploiting Allenes in Chemical Reaction Discovery"
8:35 pm - 8:45 pm Discussion
8:45 pm - 9:20 pm Jim Panek (Boston University)
"Expanding Stereochemical and Skeletal Diversity Using Chiral Organosilanes"
9:20 pm - 9:30 pm Discussion
WEDNESDAY
8:00 am - 9:00 amBreakfast
9:00 am - 12:30 pm Chemical Methodologies and Library Development
Discussion Leader: Ohyun Kwon (UCLA)
9:00 am - 9:25 am Keith Buszek (University of Missouri - Kansas City)
"Adventures in Aryne Cycloaddition Chemistry: From Natural Products Total Synthesis to Library Development"
9:25 am - 9:35 am Discussion
9:35 am - 10:00 am Alexander Doemling (University of Pittsburgh)
"Low and High Dimensional Multicomponent Reactions for Drug Discovery"
10:00 am - 10:10 am Discussion
10:10 am - 10:30 am Coffee Break
10:30 am - 10:55 am Xu Bai (Jilin University)
"Design and Synthesis of Novel Pyrimidine Fused Heterocyclic Scaffolds"
10:55 am - 11:05 am Discussion
11:05 am - 11:35 am Oliver Reiser (University of Regensburg)
"Transformation of furans and pyrrols into scaffolds for combinatorial chemistry"
11:35 am - 11:45 am Discussion
11:45 am - 12:20 pm Marvin Miller (University of Notre Dame)
"Modular Enhancement of Nature's Diversity (MEND): Nitroso Diels-Alder Reactions in Synthesis and for Facile Derivatization and Functionalization of Natural Products"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 5:00 pmPoster Session I
6:00 pmDinner
7:00 pm - 7:30 pmBusiness Meeting: Part I
(Fill out Conference Evaluation Forms; Nominations for the next Vice Chair; Discuss future Site & Scheduling preferences)
7:30 pm - 9:30 pm New Avenues in Medicinal Chemistry
Discussion Leader: Michael Walters (University of Minnesota)
7:30 pm - 8:00 pm Daniel Flynn (Deciphera Pharmaceuticals)
"Conformational-Switch Pocket Inhibitors. Biomimetic regulation of kinases by small molecules"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm Donna Huryn (University of Pennsylvania)
"A Hitchhiker's Guide to MLSCN Probe Development"
8:40 pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Sam Gerritz (Bristol-Myers Squibb)
"The Discovery and Optimization of Acyl Guanidines as Novel Inhibitors of BACE-1"
9:20 pm - 9:30 pm Discussion
THURSDAY
8:00 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness Meeting: Part II
(Vice Chair Nominee talks; Election of the next Vice Chair)
9:00 am - 12:30 pm Chemical Biology for Drug Discovery
Discussion Leader: Matt Clark (GlaxoSmithKline MDR-Boston)
9:00 am - 9:25 am Lisa Marcaurelle (Broad Institute of Harvard and MIT)
"Accessing Stereochemical and Skeletal Diversity through a Build/Couple/Pair Strategy"
9:25 am - 9:35 am Discussion
9:35 am - 10:05 am Benjamin Davis (University of Oxford)
"Sugars & Proteins: Creating Diversity in Synthetic Biology"
10:05 am - 10:15 am Discussion
10:15 am - 10:30 am Coffee Break
10:30 am - 10:55 am Lara Mahal (The University of Texas at Austin)
"A systems approach to analyzing the dynamic glycome"
10:55 am - 11:05 am Discussion
11:05 am - 11:35 am Steven Caddick (University College London)
"Diversity and Target Oriented Synthesis: Development of Synthetic Methods and Applications to Chemical Biology and Medicine"
11:35 am - 11:45 am Discussion
11:45 am - 12:20 pm Martin Semmelhack (Princeton University)
"The Chemistry of Bacterial Quorum Sensing in Cholera: the Origins of a New Therapy?"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 5:00 pmPoster Session II
5:30 pmReception on the Cloisters Lawn
6:00 pmFormal Dinner
7:30 pm - 9:30 pm Frontiers in Drug Discovery
Discussion Leader: Luis Martinez (University of Texas at El Paso)
7:30 pm - 8:00 pm Ganesan (University of Southampton)
"Cracking the Epigenetic Code"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm Chris Boss (Actelion Pharmaceuticals Ltd)
"Orexin Receptor Antagonism: A New Principle in Neuroscience"
8:40 pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Mike Foley (Broad Institute of Harvard and MIT)
"Exploiting genomic discoveries requires expanded chemical diversity"
9:20 pm - 9:30 pm Discussion
FRIDAY
8:00 am - 9:00 amBreakfast
9:00 amDeparture

Contributors

ABBOTT LABORATORIES
BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.
CEPHALON, INC.
DECIPHERA PHARMACEUTICALS LLC
ELI LILLY AND COMPANY
GENENTECH, INC.
GLAXOSMITHKLINE
MERCK & CO., INC.
SIGMA-ALDRICH
SYMYX TECHNOLOGIES
SYNGENTA LIMITED
TAKEDA SAN DIEGO, INC.

Conference Links

Conference History
Additional Fee Info

Bioorganic Chemistry
June 15 - 20, 2025
Heterocyclic Compounds
June 22 - 27, 2025
High Throughput Chemistry and Chemical Biology (GRS)
July 26 - 27, 2025
Natural Products and Bioactive Compounds
July 27 - August 1, 2025
Natural Products and Bioactive Compounds
July 28 - August 2, 2024


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