Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors

被引：36

作者：

Kitano, Yasunori

Suzuki, Tsuyoshi

Kawahara, Eiji

Yamazaki, Takahisa

机构：

[1] Mitsubishi Tanabe Pharm Corp, Med Chem Lab, Res Div, Yodogawa Ku, Osaka 5328505, Japan

[2] Mitsubishi Pharm Corp, Pharmaceut Res Div, Yokohama, Kanagawa 2270033, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 21期

关键词：

EGFR; tyrosine kinase inhibitor; 4-alkynylqumazoline; 4-alkenylquinazoline;

D O I：

10.1016/j.bmcl.2007.08.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present study identified several 4-alkynyl and 4-alkenylquinazolines that serve as novel and potent EGFR tyrosine kinase inhibitors. The IC50 values of these compounds are in the nanomolar range. In addition, the 4-(4-phenylbut-1-yl/en-yl)quinazolines provided scaffolds for potent enzyme inhibition. Chiral discrimination was observed to occur in one of the 4-alkynylquinazoline derivatives with the (R)-isomer being more than 150 times as potent as the (S)-isomer. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5863 / 5867

页数：5

共 31 条

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