Discovery of a New Class of Protein Farnesyltransferase Inhibitors in the Arylthiophene Series
- 22 September 2009
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 52 (20), 6205-6208
- https://doi.org/10.1021/jm901280q
Abstract
Screening 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.Keywords
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