Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase

被引：26

作者：

Dinsmore, CJ ^{[1
]}

Bergman, JM

Wei, DD

Zartman, CB

Davide, JP

Greenberg, IB

Liu, DM

O'Neill, TJ

Gibbs, JB

Koblan, KS

Kohl, NE

Lobell, RB

Chen, IW

McLoughlin, DA

Olah, TV

Graham, SL

Hartman, GD

Williams, TM

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

[3] Merck Res Labs, Dept Drug Metab, W Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(00)00710-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The evaluation of SAR associated with the insertion of carbonyl groups at various positions of N-arylpiperazinone farnesyltransferase inhibitors is described herein. 1-Aryl-2,3-diketopiperazine derivatives exhibited the best balance of potency and pharmacokinetic profile relative to the parent 1-aryl-2-piperazinones. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：537 / 540

页数：4

共 27 条

[1]

[Anonymous], 1983, J IMMUNOL METH

[2] Promotion of reaction of N-H bonds with triarylbismuth and cupric acetate [J].