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Article

Synthesis, activity, and their relationships of 2,4-diaminonicotinamide derivatives as EGFR inhibitors targeting C797S mutation.

Bioorganic & medicinal chemistry letters - 15 Jan 2024

Kageji Hideaki, Momose Takayuki, Nagamoto Yasuhito, Togashi Noriko, Yasumatsu Isao, Nishikawa Yosuke, Kihara Kawori, Hiramoto Kumiko, Minami Megumi, Kasanuki Naomi, Isoyama Takeshi, Naito Hiroyuki

Abstract excerpt

The C797S mutation is one of the major factors behind resistance to the third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Herein, we describe the discovery of the 2,4-diaminonicotinamide derivative 5j, which shows potent inhibitory activity against EGFR del19/T790M/C797S and L858R/T790M/C797S. We also report the structure-activity relationship of the 2,4-diaminonicotinamide...

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Identifiers

PMID: 38065292
DOI: 10.1016/j.bmcl.2023.129575

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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