Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I

被引:29
作者
Bergman, JM [1 ]
Abrams, MT
Davide, JP
Greenberg, IB
Robinson, RG
Buser, CA
Huber, HE
Koblan, KS
Kohl, NE
Lobell, RB
Graham, SL
Hartman, GD
Williams, TM
Dinsmore, CJ
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(01)00240-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of aryloxy substituted piperazinones with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to have potent inhibitory activity in vitro and are promising agents for the inhibition of Ki-Ras signaling. (C) 2001 Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1411 / 1415
页数:5
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