Synthesis and structure-activity relationships of 3-cyano-4-(phenoxyanilino)quinolines as MEK (MAPKK) inhibitors

被引：56

作者：

Zhang, N ^{[1
]}

Wu, BQ

Powell, D

Wissner, A

Floyd, MB

Kovacs, ED

Toral-Barza, L

Kohler, C

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 | 2000年 / 10卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(00)00580-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-cyano-4-(phenoxyanilino)cyanoquinolines has been prepared as MEK (MAP kinase kinase) inhibitors. The best activity is seen with alkoxy groups at both the 6- and 7-positions. The lead compounds show low nanomolar IC50's against MAP kinase kinase, and have potent inhibitory activity in tumor cells. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：2825 / 2828

页数：4

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