Article
Discovery of Potent and Wild-Type-Sparing Fourth-Generation EGFR Inhibitors for Treatment of Osimertinib-Resistance NSCLC.
Journal of medicinal chemistry - 25 May 2023
Dong Haojie, Ye Xiuquan, Zhu Yasheng, Shen Hao, Shen Hongtao, Chen Weijiao, Ji Minghui, Zheng Mingming, Wang Keren, Cai Zeyu, Sun Haopeng, Xiao Yibei, Yang Peng
Abstract excerpt
Osimertinib resistance is an unmet clinical need for the treatment of non-small cell lung cancer (NSCLC), and the main mechanism is tertiary C797S mutation of epidermal growth factor receptor (EGFR). To date, there is no inhibitor approved for the treatment of Osimertinib-resistant NSCLC. Herein, we reported a series of Osimertinib derivatives as fourth-generation inhibitors which were rationally designed. Top...
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