Article
Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer.
Journal of medicinal chemistry - 27 Apr 2023
Pei Junping, Wang Guan, Wang Aoxue, Wu Chengyong, Pan Xiaoli, Shuai Wen, Bu Faqian, Zhu Yumeng, Wang Yuxi, Ouyang Liang, Li Weimin
Abstract excerpt
Epidermal growth factor receptor (EGFR) is one of the most studied drug targets for the treatment of non-small-cell lung cancer (NSCLC). Here, we report the identification, structure optimization, and structure-activity relationship studies of quinazoline derivatives as novel selective EGFR L858R/T790M inhibitors. The most promising compound, 28f, exhibited strong inhibitory activity against EGFR L858R/T790M...
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