MEK (MAPKK) inhibitors. Part 2: Structure-activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines

被引：32

作者：

Zhang, N ^{[1
]}

Wu, BQ

Eudy, N

Wang, YN

Ye, F

Powell, D

Wissner, A

Feldberg, LR

Kim, SC

Mallon, R

Kovacs, ED

Toral-Barza, L

Kohler, CA

机构：

[1] Wyeth Ayerst Res, Chem Sci, Pearl River, NY 10965 USA

[2] Wyeth Ayerst Res, Discovery Oncol, Pearl River, NY 10965 USA

来源：

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

关键词：

D O I：

10.1016/S0960-894X(01)00238-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 4-anilino-3-cyano-6,7-dialkoxyquinolines with different substituents attached to the 4-anilino group has been prepared that are potent MEK (MAP kinase kinase) inhibitors. The best activity is obtained when a phenyl or a thienyl group is attached to the para-position of the aniline through a hydrophobic linker, such as an oxygen, a sulfur, or a methylene group. The most active compounds show low nanomolar IC50'S against MEK (MAP kinase kinase), and have potent growth inhibitory activity in LoVo cells (human colon tumor line). (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：1407 / 1410

页数：4

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