3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.
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.
D002384:Catalysis; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D007211:Indoles / Q000494:pharmacology*; D007700:Kinetics; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D007211:Indoles; D007168:IMP Dehydrogenase