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

…, C Davis, W Long, Y Hu, F Wang, X Kang, F Tan…

文献索引：Hu, Shaojing; Xie, Guojian; Zhang, Don X.; Davis, Charles; Long, Wei; Hu, Yunyan; Wang, Fei; Kang, Xinshan; Tan, Fenlai; Ding, Lieming; Wang, Yinxiang Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 19 p. 6301 - 6305

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被引用次数: 28

摘要

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 ...