2. Academic Validation
  3. 3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships

3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships

  • Bioorg Med Chem Lett. 2003 Oct 20;13(20):3557-60. doi: 10.1016/s0960-894x(03)00757-1.
T G Murali Dhar 1,  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
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. [email protected]
PMID: 14505670 DOI: 10.1016/s0960-894x(03)00757-1
Abstract

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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