Structure-Guided Design of C4-alkyl-1,4-dihydro-2H-pyrimido[4,5-d][1,3]oxazin-2-ones as Potent and Mutant-Selective Epidermal Growth Factor Receptor (EGFR) L858R/T790M Inhibitors

Epidermal growth factor receptor (EGFR) T790M acquired drug-resistance mutation has become a major clinical challenge for the therapy of non-small cell lung cancer. Here, we applied a structure-guided approach on the basis of the previous reported EGFR inhibitor (compound 9), and designed a series o...

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Published in:Sci Rep
Main Authors: Hao, Yongjia, Lyu, Jiankun, Qu, Rong, Sun, Deheng, Zhao, Zhenjiang, Chen, Zhuo, Ding, Jian, Xie, Hua, Xu, Yufang, Li, Honglin
Format: Artigo
Language:Inglês
Published: Nature Publishing Group UK 2017
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Article
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC5476563/
https://ncbi.nlm.nih.gov/pubmed/28630494
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41598-017-04184-9
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