jm901280q_si_001.pdf (231.37 kB)
Discovery of a New Class of Protein Farnesyltransferase Inhibitors in the Arylthiophene Series
journal contribution
posted on 2009-10-22, 00:00 authored by Sébastien Lethu, Maryon Ginisty, Damien Bosc, Joëlle DuboisScreening of the ICSN chemical library led to the discovery of 3-(4-chlorophenyl)-4-cyano-5-thioalkylthiophene 2-carboxylic acids as potent farnesyltransferase inhibitors. Enzymatic kinetic studies showed that this original FTI series belongs to the CaaX competitive inhibitor class. Preliminary SAR studies allowed us to improve the IC50 from 110 to 7.5 nM.