Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor

被引：18

作者：

Carolina, A

Sosa, B

Boschelli, DH

Wu, BQ

Wang, Y

Golas, JM

机构：

[1] Roche Carolina Inc, Pharmaceut Proc Dev, Florence, SC 29506 USA

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 06期

关键词：

Src; kinase; 3-quinolinecarbonitriles;

D O I：

10.1016/j.bmcl.2005.01.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several new ethynyl- and ethenyl-4-phenylamino-3-quinolinecarbonitriles were synthesized and tested for Src inhibition. Derivatives bearing an ethenyl or ethynyl substituent at C-6 showed decreased Src inhibitory activity. Incorporation of an ethenylpyridine N-oxide group at C-7 provided 20b, a 0.6 nM inhibitor of Src enzymatic activity with excellent cellular potency. (c) 2005 Published by Elsevier Ltd.

引用

页码：1743 / 1747

页数：5

共 14 条

[11] Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles [J].