Novel tricyclic aminoacetyl and sulfonamide inhibitors of ras farnesyl protein transferase

Article abstract of DOI:10.1016/S0960-894X(96)00558-6

Novel tricyclic FPT inhibitors with submicromolar FPT activity are described. Greatly enhanced FPT activity is realized with phthaloyl derivatized amino compound 2k, which showed FPT inhibitory activity of IC₅₀ = 0.66 μM. Sulfonamides 5g and 50 were also found to be potent FPT inhibitor. SAR resulting from a variety of tricyclic amino acids and sulfonamide derivatives is discussed.