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Article

Discovery of a potent, selective, and orally available EGFR C797S mutant inhibitor (DS06652923) with in vivo antitumor activity.

Bioorganic & medicinal chemistry - 1 Sept 2024

Kageji Hideaki, Momose Takayuki, Ebisawa Masayuki, Nakazawa Yusuke, Okada Hiroyuki, Togashi Noriko, Nagamoto Yasuhito, Obuchi Wataru, Yasumatsu Isao, Kihara Kawori, Hiramoto Kumiko, Minami Megumi, Kasanuki Naomi, Isoyama Takeshi, Naito Hiroyuki, Tanaka Naoki

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 (TKIs). Herein, we describe the discovery of DS06652923, a novel, potent, and orally available EGFR-triple-mutant inhibitor. Through scaffold hopping from the previously reported nicotinamide derivative, a novel biaryl scaffold was obtained. The potency was...

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Identifiers

PMID: 39111073
DOI: 10.1016/j.bmc.2024.117862

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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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