Article
Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S).
Bioorganic & medicinal chemistry letters - 15 Sept 2022
Fang Haotian, Wu Yingming, Xiao Qitao, He Dongbo, Zhou Tongrui, Liu Wenzhong, Yang Chun-Hao, Xie Yuli
Abstract excerpt
Although epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) have demonstrated encouraging clinical outcomes for patients with EGFR-mutated non-small cell lung cancer, a considerable number of patients will develop drug resistance and eventually undergo disease progression after taking EGFR-TKIs for a period of time. EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S are two most prevalent...
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