Article
Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant.
Bioorganic & medicinal chemistry - 15 Mar 2021
Fukuda Tsutomu, Anzai Mizuho, Nakahara Akane, Yamashita Kentaro, Matsukura Kazuaki, Ishibashi Fumito, Oku Yusuke, Nishiya Naoyuki, Uehara Yoshimasa, Iwao Masatomo
Abstract excerpt
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 tyrosine kinase assay indicated that the inhibitory activities of the synthetic azalamellarin analogues were higher than those of the...
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