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Design, synthesis, and biological evaluation of 2-arylamino-4-(piperidin-4-yloxy)pyrimidines as potent EGFRT790M/L858R inhibitors to treat non-small cell lung cancer.

Bioorganic & medicinal chemistry - 15 Nov 2022

Tian Liangliang, Li Xing, Lv Zhenying, Yang Yin, Wang Luhong, Xu Dawei, Ma Xiaodong, Xu Youjun

Abstract excerpt

Three types of 2-arylamino-4-(piperidin-4-yloxy)pyrimidines (I-III) were designed and synthesized as covalent EGFR(epidermal growth factor receptor)T790M/L858R inhibitors by replacement of the common reported 4-(3-amino)phenoxyl moiety with 4-(4-hydroxy)piperidine-4-oxyl, and the introduction of fused-thiophene or -pyrrole on the pyrimidine core to strategically achieve conformational restriction. According to...

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PMID: 36288657
DOI: 10.1016/j.bmc.2022.117052

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