Article
Design, synthesis and biological evaluation of 2,4,5-trisubstituted 7H-Pyrrolo[2,3-d]pyrimidine derivatives as potent EGFR tyrosine kinase inhibitors against the C797S acquired resistance mutation.
Bioorganic & medicinal chemistry - 1 Aug 2026
Zhang Hao, Lan Tianlong, Li Rui, Li Guangyan, Yuan Jiang, Wang Songning, Zhang Zhenjun, Zhang Zhenyu, Liu Jing, Liu Hua, Xu Lijuan, Li Yuting, Pan Sina, Pan Lihong, Wang Xishuang, Wang Xianzhen, Xu Xiaoli, Xiao He, Wen Yixiao, Wang Enli, Zhao Tao, Sun Jingxia, Wang Peng, Qiu Rongying, Li Tao, Yao Jingchun, Liu Zhong, Zhang Guimin
Abstract excerpt
The C797S mutation in the epidermal growth factor receptor (EGFR) presents a significant challenge in treating non-small cell lung cancer (NSCLC), as it confers resistance to osimertinib. To tackle this issue, we designed and synthesized novel 7H-pyrrolo[2,3-d]pyrimidine derivatives that bind to the EGFR kinase domain in the presence of the C797S mutation. The representative compound cis-32 (LN-B72) not only...
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