Article
Structure-guided discovery of a potent 2-aryl-4-aminoquinazoline-based inhibitor overcoming osimertinib resistance driven by EGFR C797S mutation in NSCLC.
European journal of medicinal chemistry - 5 Jul 2026
Chang Hao, Zhang Cheng, Liang Zhenyang, Liu Fang, Zhang Yanhong, Tian Jiaxin, Xiao Zijie, Chi Haohua, Du Wenwen, Li Shu, Li Pengmei, Qiao Renzhong, Li Chao
Abstract excerpt
The C797S mutation in epidermal growth factor receptor (EGFR) is a major mechanism of resistance to third-generation tyrosine kinase inhibitors (TKIs), such as Osimertinib, in non-small cell lung cancer (NSCLC), creating an urgent need for effective therapeutic strategies. To address this challenge, we designed the structure-guided optimization of a 2-aryl-4-aminoquinazoline scaffold, leading to the discovery of...
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