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3-Cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure–Activity relationships

✍ Scribed by T.G. Murali Dhar; Zhongqi Shen; Henry H. Gu; Ping Chen; Derek Norris; Scott H. Watterson; Shelley K. Ballentine; Catherine A. Fleener; Katherine A. Rouleau; Joel C. Barrish; Robert Townsend; Diane L. Hollenbaugh; Edwin J. Iwanowicz

Publisher: Elsevier Science
Year: 2003
Tongue: English
Weight: 186 KB
Volume: 13
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(03)00757-1

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✦ Synopsis

A series of novel small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH), based upon a 3-cyanoindole core, were explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SAR), derived from in vitro studies, for this new series of inhibitors is given.

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