Article
Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors.
European journal of medicinal chemistry - 5 Aug 2022
Ding Shi, Gao Ziye, Hu Ziqiang, Qi Rui, Zheng Xiangshan, Dong Xiaoyong, Zhang Mingjuan, Shen Jiwei, Long Tian, Zhu Yan, Tian Lu, Song Wenshan, Liu Ruoqing, Li Ying, Sun Jiahuan, Duan Wenwen, Liu Ju, Chen Ye
Abstract excerpt
A series of osimertinib derivatives without acrylamide groups were synthesized and their inhibitory rates against L858R/T790M/C797S mutated EGFR kinase and antiproliferation activities against non-small cell lung cancer cell lines (A549, H1975) were evaluated. The preferred compounds were selected and their in vitro inhibitory activities against various EGFR kinases (wild-type, L858R/T790M, L858R/T790M/C797S) and...
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