Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I

被引：9

作者：

Dinsmore, CJ ^{[1
]}

Zartman, CB

Bergman, JM

Abrams, MT

Buser, CA

Culberson, JC

Davide, JP

Ellis-Hutchings, M

Fernandes, C

Graham, SL

Hartman, GD

Huber, HE

Lobell, RB

Mosser, SD

Robinson, RG

Williams, TM

机构：

[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA

[2] Merck Res Labs, Dept Canc Res, West Point, PA 19486 USA

[3] Merck Res Labs, Dept Mol Syst, West Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

inhibitor; farnesyltransferase; geranylgernyltransferase;

D O I：

10.1016/j.bmcl.2003.11.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of macrocyclic piperazinone compounds with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to be potent inhibitors of protein prenylation in cell culture. A hypothesis for the binding mode of compound 3o in FPTase is proposed. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：639 / 643

页数：5

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