Potent, non-thiol inhibitors of farnesyltransferase

被引:31
作者
Breslin, MJ [1 ]
deSolms, SJ
Giuliani, EA
Stokker, GE
Graham, SL
Pompliano, DL
Mosser, SD
Hamilton, KA
Hutchinson, JH
机构
[1] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA
[2] Merck Res Labs, Dept Canc Res, W Point, PA 19486 USA
关键词
D O I
10.1016/S0960-894X(98)00586-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The structure-activity relationship of a series of non-thiol CaaX analogs, which are inhibitors of farnesyltransferase, is described. These inhibitors contain a substituted phenyl group at the N terminus, which may occupy a novel binding domain on the Ras protein. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3311 / 3316
页数:6
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