Synthesis and evaluation of 2, 7-diamino-thiazolo [4, 5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

…, WV Murray, NB Pandey, SJ Moreno-Mazza…

文献索引：Lin, Ronghui; Johnson, Sigmond G.; Connolly, Peter J.; Wetter, Steven K.; Binnun, Eva; Hughes, Terry V.; Murray, William V.; Pandey, Niranjan B.; Moreno-Mazza, Sandra J.; Adams, Mary; Fuentes-Pesquera, Angel R.; Middleton, Steven A. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 8 p. 2333 - 2337

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被引用次数: 78

摘要

2, 7-Diamino-thiazolo [4, 5-d] pyrimidine analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities and inhibited in vitro cellular proliferation in EGFR-overexpressing human tumor cells. The synthesis and preliminary biological, physical, and pharmacokinetic evaluation of these thiazolopyrimidine ...