Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase

被引：81

作者：

Dinsmore, CJ ^{[1
]}

Williams, TM

O'Neill, TJ

Liu, DM

Rands, E

Culberson, JC

Lobell, RB

Koblan, KS

Kohl, NE

Gibbs, JB

Oliff, AI

Graham, SL

Hartman, GD

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 Mol Syst, W Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(99)00605-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design and syntheses of non-thiol inhibitors of farnesyl-protein transferase are described. Optimization of cysteine-substituted diarylethers led to highly potent imidazole-containing diarylethers and diarylsulfones. Polar diaryl linkers dramatically improved potency and gave highly cell active compounds. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：3301 / 3306

页数：6

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