Article
Design, synthesis and biological evaluation of EGFR kinase inhibitors that spans the orthosteric and allosteric sites.
Bioorganic & medicinal chemistry - 15 Dec 2023
Fan Mengmeng, Hu Liping, Shi Shengmin, Song Xiaomeng, He Huan, Qi Baohui
Abstract excerpt
Acquired drug resistance occurred in the treatment of non-small-cell lung cancer is a persistent challenge, especially in EGFR mutant type. In this study, we present design, synthesis and biological evaluation of novel quinazoline and pyrrolopyrimidine derivatives that simultaneously occupy the orthosteric and allosteric sites of EGFR. Among them, compound A-7 was confirmed as a potential EGFRL858R/T790M/C797S...
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