Continuing structure-activity studies were performed on the 2, 3, 4, 5-tetrahydro-1-(imidazol- 4-ylalkyl)-1, 4-benzodiazepine farnesyltransferase (FT) inhibitors. These studies demonstrated that a 3 (R)-phenylmethyl group, a hydrophilic 7-cyano group, and a 4- sulfonyl group bearing a variety of substituents provide low-nanomolar FT inhibitors with cellular activity at concentrations below 100 nM. Maximal in vivo activity in the mutated K- ...
