7-IMIDAZOLYLALKANAMIDO-1-CARBOXYLALKYLBENZO-DIAZEPINE, A NOVEL SERIES OF FARNESYLTRANSFERASE INHIBITORS

AIMDesign, synthesis and evaluation of a series of 7-imidazolylalkanamido-1-carboxylalkylbenzodiazepine farnesyltransferase (FTase) inhibitors. METHODS and RESULTSCoupling of imidazolylalkylcarboxylic acids and 1-substituted 7-aminobenzodiazepines (5a～5c) yielded 10 new compounds (6～12, 16～18) which were biologically tested against FTase using scintillation proximity assay method. CONCLUSIONFive target compounds were found to be potential farnesyltransferase inhibitors.