Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors

被引：16

作者：

Boschelli, Diane H. ^{[1
]}

Wang, Daniel ^{[1
]}

Wang, Yan ^{[1
]}

Wu, Biqi ^{[1
]}

Honores, Erick E. ^{[1
]}

Sosa, Ana Carolina Barrios ^{[1
]}

Chaudhary, Inder ^{[1
]}

Golas, Jennifer ^{[1
]}

Lucas, Judy ^{[1
]}

Boschelli, Frank ^{[1
]}

机构：

[1] Wyeth Res, Pearl River, NY 10965 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 09期

关键词：

3-Quinolinecarbonitrile; Src; Kinase; THERAPEUTIC TARGETS; TYROSINE KINASE; ABL; 4-PHENYLAMINO-3-QUINOLINECARBONITRILES;

D O I：

10.1016/j.bmcl.2010.03.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC50 values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study. (C) 2010 Elsevier Ltd. All rights reserved.

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收藏

页码：2924 / 2927

页数：4

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