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Discovery of new [1,4]dioxino[2,3-f]quinazoline-based inhibitors of EGFR including the T790M/L858R mutant.

Bioorganic & medicinal chemistry - 1 Jul 2016

Qin Xuemei, Li Zhipeng, Yang Leifu, Liu Peng, Hu Liming, Zeng Chengchu, Pan Zhiyong

Abstract excerpt

A novel series of 2,3-dihydro-[1,4]dioxino[2,3-f]quinazoline derivatives were designed, synthesized and evaluated as reversible and noncovalent epidermal growth factor receptor (EGFR) inhibitors. Most of the compounds exhibited good potency against EGFR(wt) and some showed moderate to excellent potency against EGFR(T790M/L858R) mutant. The half-maximal inhibitory concentration (IC50) values of twenty-one...

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Identifiers

PMID: 27234887
DOI: 10.1016/j.bmc.2016.01.003

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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