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Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant
http://hdl.handle.net/10069/00040535
http://hdl.handle.net/10069/0004053573d42ef6-3bb7-4938-8a79-b5a805e59cb2
名前 / ファイル | ライセンス | アクション |
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BMChem34_116039.pdf (7.0 MB)
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supplementary data.pdf (6.7 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2021-01-23 | |||||
タイトル | ||||||
タイトル | Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | A-ring-modified azalamellarin analogues | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Azalamellarin N | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | EGFR T790M/L858R mutant | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | EGFR tyrosine kinase inhibitors (EGFR-TKIs) | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
Fukuda, Tsutomu
× Fukuda, Tsutomu× Anzai, Mizuho× Nakahara, Akane× Yamashita, Kentaro× Matsukura, Kazuaki× Ishibashi, Fumito× Oku, Yusuke× Nishiya, Naoyuki× Uehara, Yoshimasa× Iwao, Masatomo |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | 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. | |||||
書誌情報 |
Bioorganic & Medicinal Chemistry 巻 34, p. 116039, 発行日 2021-01-23 |
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出版者 | ||||||
出版者 | Elevier Ltd | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 09680896 | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.bmc.2021.116039 | |||||
権利 | ||||||
権利情報 | © 2021 Elsevier Ltd. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ | |||||
著者版フラグ | ||||||
出版タイプ | AM | |||||
出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||
引用 | ||||||
内容記述タイプ | Other | |||||
内容記述 | Bioorganic and Medicinal Chemistry, 34, art.no.116039; 2021 |