Discovery of a New Class of Protein Farnesyltransferase Inhibitors in the Arylthiophene Series

被引：29

作者：

Lethu, Sebastien ^{[1
]}

Ginisty, Maryon ^{[1
]}

Bosc, Damien ^{[1
]}

Dubois, Joelle ^{[1
]}

机构：

[1] CNRS, Ctr Rech Gif sur Yvette, Inst Chim Subst Nat, UPR2301, F-91198 Gif Sur Yvette, France

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 20期

关键词：

THIOPHENES;

D O I：

10.1021/jm901280q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 its to improve the IC50 from 110 to 7.5 nM.

引用

页码：6205 / 6208

页数：4

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