Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.

Shaojing Hu,Guojian Xie,Don X Zhang,Charles Davis,Wei Long,Yunyan Hu,Fei Wang,Xinshan Kang,Fenlai Tan,Lieming Ding,Yinxiang Wang

Bioorganic & Medicinal Chemistry Letters（2013）

引用 69|浏览12

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摘要

A series of crown ether fused anilinoquinazolines have been synthesized and evaluated for EGFR inhibition. Compound 12k (Icotinib) showed excellent enzymatic and cellular activities against EGFR. Icotinib is in phase III clinical trials currently.

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关键词

EGFR inhibitor,Crown ether fused anilinoquinazoline,Synthesis

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