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Distributed Drug Discovery, Part 3: Using D3 Methodology to Synthesize Analogs of an Anti-Melanoma Compound
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Hi-Res PDFIndiana University−Purdue University Indianapolis.
, #Eli Lilly and Company.
Section:Abstract
For the successful implementation of Distributed Drug Discovery (D3) (outlined in the accompanying Perspective), students, in the course of their educational laboratories, must be able to reproducibly make new, high quality, molecules with potential for biological activity. This article reports the successful achievement of this goal. Using previously rehearsed alkylating agents, students in a second semester organic chemistry laboratory performed a solid-phase combinatorial chemistry experiment in which they made 38 new analogs of the most potent member of a class of antimelanoma compounds. All compounds were made in duplicate, purified by silica gel chromatography, and characterized by NMR and LC/MS. As a continuing part of the Distributed Drug Discovery program, a virtual D3 catalog based on this work was then enumerated and is made freely available to the global scientific community.
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This article has been cited by 4 ACS Journal articles (4 most recent appear below).
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Solid-Phase Synthesis of Amino- and Carboxyl-Functionalized Unnatural α-Amino Acid Amides
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William L. Scott, Ziniu Zhou, Jacek G. Martynow and Martin J. O’DonnellOrganic Letters2009 11 (16), 3558-3561A new solid-phase synthesis efficiently incorporates three different substituents (from R1-X, R2-CO2H, and R3-NH2) into a glycine-based peptidomimetic scaffold. The synthetic sequence is general and is typically accomplished in >50% overall isolated ...
Distributed Drug Discovery, Part 1: Linking Academia and Combinatorial Chemistry to Find Drug Leads for Developing World Diseases
William L. Scott and Martin J. O’DonnellJournal of Combinatorial Chemistry2009 11 (1), 3-13Distributed Drug Discovery, Part 1: Linking Academia and Combinatorial Chemistry to Find Drug Leads for Developing World Diseases
William L. Scott and Martin J. O’DonnellJournal of Combinatorial Chemistry2009 11 (1), 3-13
Distributed Drug Discovery, Part 2: Global Rehearsal of Alkylating Agents for the Synthesis of Resin-Bound Unnatural Amino Acids and Virtual D3 Catalog Construction
William L. Scott, Jordi Alsina, Christopher O. Audu, Evgenii Babaev, Linda Cook, Jeffery L. Dage, Lawrence A. Goodwin, Jacek G. Martynow, Dariusz Matosiuk, Miriam Royo, Judith G. Smith, Andrew T. Strong, Kirk Wickizer, Eric M. Woerly, Ziniu Zhou and Martin J. O’DonnellJournal of Combinatorial Chemistry2009 11 (1), 14-33Distributed Drug Discovery, Part 2: Global Rehearsal of Alkylating Agents for the Synthesis of Resin-Bound Unnatural Amino Acids and Virtual D3 Catalog Construction
William L. Scott, Jordi Alsina, Christopher O. Audu, Evgenii Babaev, Linda Cook, Jeffery L. Dage, Lawrence A. Goodwin, Jacek G. Martynow, Dariusz Matosiuk, Miriam Royo, Judith G. Smith, Andrew T. Strong, Kirk Wickizer, Eric M. Woerly, Ziniu Zhou and Martin J. O’DonnellJournal of Combinatorial Chemistry2009 11 (1), 14-33Distributed Drug Discovery (D3) proposes solving large drug discovery problems by breaking them into smaller units for processing at multiple sites. A key component of the synthetic and computational stages of D3 is the global rehearsal of prospective ...
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History
- Published In Issue January 12, 2009
- Article ASAPDecember 23, 2008
- Received: November 14, 2008
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