Author/Authors :
T. G. Murali Dhar، نويسنده , , Zhongqi Shen، نويسنده , , Henry H. Gu، نويسنده , , Ping Chen، نويسنده , , Derek Norris، نويسنده , , Scott H. Watterson، نويسنده , , Shelley K. Ballentine، نويسنده , , Catherine A. Fleener، نويسنده , , Katherine A. Rouleau، نويسنده , , Joel C. Barrish، نويسنده , , Robert Townsend، نويسنده , , Diane L. Hollenbaugh، نويسنده , , Edwin J. Iwanowicz، نويسنده ,
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.