Article
Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors.
European journal of medicinal chemistry - 15 Jan 2020
Lei Hao, Fan Shu, Zhang Hao, Liu Yan-Jie, Hei Yuan-Yuan, Zhang Jun-Jie, Zheng A-Qun, Xin Minhang, Zhang San-Qi
Abstract excerpt
Targeting L858R/T790M/C797S mutant EGFR is a major challenge in the new-generation EGFR tyrosine kinase inhibitors development for conquering drug resistant NSCLC. In this study, a series of novel 9-heterocyclyl substituted 9H-purine derivatives were designed as EGFRL858 R/T790 M/C797S tyrosine kinase inhibitors. Among these compounds, D4, D9, D11 and D12 showed significantly potent anti-proliferation and...
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