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Article

Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant.

Bioorganic & medicinal chemistry - 15 Dec 2017

Fukuda Tsutomu, Umeki Teppei, Tokushima Keiji, Xiang Gao, Yoshida Yuki, Ishibashi Fumito, Oku Yusuke, Nishiya Naoyuki, Uehara Yoshimasa, Iwao Masatomo

Abstract excerpt

A series of A-ring-modified lamellarin N analogues were designed, synthesized, and evaluated as potential noncovalent inhibitors of the EGFR T790M/L858R mutant, a causal factor in the drug-resistant non-small cell lung cancer. Several water-soluble ammonium- or guanidinium-tethered analogues exhibited good kinase inhibitory activities. The most promising analogue, 14f, displayed an excellent inhibitory profile...

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Identifiers

PMID: 29133033
DOI: 10.1016/j.bmc.2017.10.030

Genes

EGFR

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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