Article
Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment.
European journal of medicinal chemistry - 5 Jul 2022
Wang Cheng, Wang Xin, Huang Zhi, Wang Tianqi, Nie Yongwei, Yang Shengyong, Xiang Rong, Fan Yan
Abstract excerpt
The C797S mutation in EGFR is a leading mechanism of clinically acquired resistance against osimertinib for non-small cell lung cancer (NSCLC). In this study, we identified a potent and oral EGFRL858R/T790M/C797S tyrosine kinase inhibitor, 14aj with a novel chemical scaffold. Compound 14aj showed low nanomolar activity against EGFRL858R/T790M/C797S mutant with IC50 value as 0.010 μM. In vitro assays, compound...
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