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Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant
http://hdl.handle.net/10069/38936
http://hdl.handle.net/10069/3893691d184cb-6556-425e-b3a0-22e29dc47b64
名前 / ファイル | ライセンス | アクション |
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Supplementary_data.pdf (17.3 MB)
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BMC25_6563.pdf (1.7 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2019-12-15 | |||||
タイトル | ||||||
タイトル | Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | EGFR tyrosine kinase inhibitors (EGFR-TKI) | |||||
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 | Structure-based drug design (SBDD) | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Lamellarin N | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Water-soluble analogues | |||||
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× Umeki, Teppei× Tokushima, Keiji× Xiang, Gao× Yoshida, Yuki× 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 | 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 against the T790M/L858R mutant [IC50 (WT)?=?31.8?nM; IC50 (T790M/L858R)?=?8.9?nM]. The effects of A-ring-substituents on activity were rationalized by docking studies. | |||||
書誌情報 |
Bioorganic & Medicinal Chemistry 巻 25, 号 24, p. 6563-6580, 発行日 2017-12-15 |
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出版者 | ||||||
出版者 | Elsevier 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.2017.10.030 | |||||
権利 | ||||||
権利情報 | c2017, Elsevier. 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 & Medicinal Chemistry, 25(24), pp.6563-6580; 2017 |