Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles

被引：16

作者：

Sosa, ACB

Boschelli, DH

Ye, F

Golas, JM

Boschelli, F

机构：

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 09期

关键词：

Src kinase; Src inhibitors; kinase inhibitors; tyrosine kinase; quinolinecarbonitriles;

D O I：

10.1016/j.bmcl.2004.02.035

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 7-ethynyl and 7-ethenyl-4-anilino-3-quinolinecarbonitriles were synthesized and tested for Src inhibition. Derivatives bearing a C-6 methoxy group and 2,4-dichloro-5-methoxyaniline at C-4 showed optimal inhibition of Src enzymatic and cellular activity. The ethenyl and ethynyl groups were incorporated at C-7 utilizing a Stille, Heck, or Sonogashira coupling reaction. (C) 2004 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2155 / 2158

页数：4

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