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

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Dhar TG, Shen Z, Gu HH, Chen P, Norris D, Watterson SH, Ballentine SK, Fleener CA, Rouleau KA, Barrish JC, Townsend R, Hollenbaugh DL, Iwanowicz EJ

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.

PubMed ID

14505670 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mycophenolic acid	Inosine-5'-monophosphate dehydrogenase 2	IC 50 (nM)	15	N/A	N/A	Details