Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors

被引：45
|
作者：
Pannala, Madhavi
Kher, Sunil
Wilson, Norma
Gaudette, John
Sircar, Ila
Zhang, Shao-Hul
Bakhirev, Alexei
Yang, Guang
Yuen, Phoebe
Gorcsan, Frank
Sakurai, Naoki
Barbosa, Miguel
Cheng, Jie-Fei
机构：
[1] Tanabe Res Lab USA Inc, Dept Chem, San Diego, CA 92121 USA
[2] Tanabe Res Lab USA Inc, Dept Biol, San Diego, CA 92121 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 21期
关键词：
EGFR inhibitor; quinoline-3-carbonitrile;
D O I：
10.1016/j.bmcl.2007.07.071
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Synthesis and structure-activity relationship of a series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitrile derivatives as EGFR inhibitors is described. Compounds 29 and 30 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the functional cellular assay. They are moderately selective against other types of tyrosine kinases. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5978 / 5982
页数：5
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