Syntheses of 4-(indole-3-yl)quinazolines -: A new class of epidermal growth factor receptor tyrosine kinase inhibitors

被引：108

作者：

Lueth, Anja ^{[1
]}

Loewe, Wemer ^{[1
]}

机构：

[1] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 43卷 / 07期

关键词：

tyrosine kinase inhibitors; EGFR; HER-2; ATP antagonist;

D O I：

10.1016/j.ejmech.2007.09.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The epidermal growth factor (EGF) family of membrane receptors has been identified as a key element in the complex signaling network that is utilized by various classes of cell-surface receptors. The synthesis and pharmacological results of 4-(indole-3-yl)quinazolines are described. The synthesized compounds are new high potent EGFR-tyrosine kinase inhibitors with excellent cytotoxic properties at different cell lines. Furthermore the 4-(indole-3-yl)quinazolines show some tendencies to inhibit the HER-2 TK, too. Moreover this substance class has remarkable strong fluorescence properties. (c) 2007 Elsevier Masson SAS. All rights reserved.

引用

页码：1478 / 1488

页数：11

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