Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors
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- 作者：Shaojing Hu ; Guojian Xie ; Don X. Zhang ; Charles Davis ; Wei Long ; Yunyan Hu ; Fei Wang ; Xinshan Kang ; Fenlai Tan ; Lieming Ding ; Yinxiang Wang
- 关键词：EGFR inhibitor ; Crown ether fused anilinoquinazoline ; Synthesis
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：1 October, 2012
- 年：2012
- 卷：22
- 期：19
- 页码：6301-6305
- 全文大小：723 K
文摘
Crown ether fused anilinoquinazoline analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities in an in vitro EGFR kinase assay and an EGFR-mediated intracellular tyrosine phosphorylation assay. The synthesis and preliminary biological, physical, and pharmacokinetic evaluation of these fused quinazoline compounds is reported.