Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant

[Display omitted] Azalamellarin N, a synthetic lactam congener of the marine natural product lamellarin N, and its A-ring-modified analogues were synthesized and evaluated as potent and non-covalent inhibitors of the drug-resistant epidermal growth factor receptor T790M/L858R mutant. An in vitro tyr...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2021-03, Vol.34, p.116039-116039, Article 116039
Hauptverfasser:	Fukuda, Tsutomu, Anzai, Mizuho, Nakahara, Akane, Yamashita, Kentaro, Matsukura, Kazuaki, Ishibashi, Fumito, Oku, Yusuke, Nishiya, Naoyuki, Uehara, Yoshimasa, Iwao, Masatomo
Format:	Artikel
Sprache:	eng
Schlagworte:	A-ring-modified azalamellarin analogues Azalamellarin N EGFR T790M/L858R mutant EGFR tyrosine kinase inhibitors (EGFR-TKIs)
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