@article{oai:nagasaki-u.repo.nii.ac.jp:00026337,
 author = {Fukuda, Tsutomu and Anzai, Mizuho and Nakahara, Akane and Yamashita, Kentaro and Matsukura, Kazuaki and Ishibashi, Fumito and Oku, Yusuke and Nishiya, Naoyuki and Uehara, Yoshimasa and Iwao, Masatomo},
 journal = {Bioorganic & Medicinal Chemistry},
 month = {Jan},
 note = {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 corresponding lamellarins.The azalamellarin analogue bearing two 3-(dimethylamino)propoxy groups at C20- and C21-positions exhibited the highest activity and selectivity against the mutant kinase [IC50 (T790M/L858R) = 1.7 nM; IC50 (WT) = 4.6 nM]. The inhibitory activity was attributed to the hydrogen bonding interaction between the lactam NH group of the B-ring and carbonyl group of a methionine residue., Bioorganic and Medicinal Chemistry, 34, art.no.116039; 2021},
 title = {Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant},
 volume = {34},
 year = {2021}
}