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Article

Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold.

Bioorganic & medicinal chemistry - 1 May 2018

Hu Jinxing, Han Yufei, Wang Jingtao, Liu Yue, Zhao Yanfang, Liu Yajing, Gong Ping

Abstract excerpt

Based upon the modeling binding mode of marketed AZD9291 with T790M, a series of N-9-Diphenyl-9H-purin-2-amine derivatives were designed and synthesized with the purpose to overcome the drug resistance resulted from T790M/L858R double mutations. The most potent compound 23a showed excellent enzyme inhibitory activities and selectivity with nanomolar IC50 values for both the single T790M and double T790M/L858R...

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Identifiers

PMID: 29486953
DOI: 10.1016/j.bmc.2018.02.029

Genes

EGFR

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