Author/Authors :
Diem N. Nguyen، نويسنده , , Craig A. Stump، نويسنده , , Eileen S. Walsh، نويسنده , , Christine Fernandes، نويسنده , , Joseph P. Davide، نويسنده , , Michelle Ellis-Hutchings، نويسنده , , Ronald G. Robinson، نويسنده , , Theresa M. Williams، نويسنده , , Robert B. Lobell، نويسنده , , Hans E. Huber، نويسنده , , Carolyn A. Buser، نويسنده ,
Abstract :
Compound 1 has been shown to be a dual prenylation inhibitor with FPTase (IC50=2 nM) and GGPTase-I (IC50=95 nM). Analogues of 1, which replaced the cyanophenyl group with various biaryls, led to the discovery of highly potent dual FPTase/GGPTase-I inhibitors. 4-Trifluoromethylphenyl, trifluoropentynyl, and trifluoropentyl were identified as good p-cyano replacements.
