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Article

Discovery of N-aryl-N'-pyrimidin-4-yl ureas as irreversible L858R/T790M mutant selective epidermal growth factor receptor inhibitors.

Bioorganic & medicinal chemistry letters - 15 Apr 2018

Zhou Fusheng, Zhang Liang, Jin Yunzhou, Liu Wei, Cheng Pengfei, He Xiangyu, Xie Jing, Shen Sida, Lei Jing, Ji Haixia, Hu Yi, Liu Yingtao, Cui Yumin, Lv Qiang, Lan Jiong

Abstract excerpt

A novel series of N-aryl-N'-pyrimidin-4-yl ureas has been optimized to afford potent and selective inhibitors of the EGFR L858R/T790M. The most representative compound 28 showed high activity against EGFR L858R/T790M kinase (IC50 = 4 nM) and 22-fold selectivity against wild type EGFR. Moreover, compound 28 potently inhibited EGFR L858R/T790M phosphorylation (IC50 = 41 nM) and cellular proliferation (IC50 = 37 nM)...

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Identifiers

PMID: 29534926
DOI: 10.1016/j.bmcl.2017.12.009

Genes

EGFR

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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