Novel tricyclic aminoacetyl and sulfonamide inhibitors of Ras farnesyl protein transferase
作者:F.George Njoroge、Bancha Vibulbhan、Carmen S. Alvarez、W.Robert Bishop、Joanne Petrin、Ronald J. Doll、V. Girijavallabhan、Ashit K. Ganguly
DOI:10.1016/s0960-894x(96)00558-6
日期:1996.12
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 mu M. 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. Copyright (C) 1996 Elsevier Science Ltd