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Combinatorial Synthesis and Biological Evaluation of Destruxins
http://hdl.handle.net/2241/00159754
http://hdl.handle.net/2241/001597546006c93b-b3b9-4904-b500-a8c298e846b2
名前 / ファイル | ライセンス | アクション |
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CPB_67-10 (1.1 MB)
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Item type | Journal Article(1) | |||||||||||
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公開日 | 2020-03-17 | |||||||||||
タイトル | ||||||||||||
言語 | en | |||||||||||
タイトル | Combinatorial Synthesis and Biological Evaluation of Destruxins | |||||||||||
言語 | ||||||||||||
言語 | eng | |||||||||||
資源タイプ | ||||||||||||
資源 | http://purl.org/coar/resource_type/c_6501 | |||||||||||
タイプ | journal article | |||||||||||
著者 |
吉田, 将人
× 吉田, 将人
WEKO
205035
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抄録 | ||||||||||||
内容記述タイプ | Abstract | |||||||||||
内容記述 | The combinatorial synthesis and biological evaluation of destruxins are described herein. First, the total synthesis of destruxin E was achieved, and its absolute configuration was successfully determined to be (S). In addition, the preparation of a combinatorial library based on the structure of destruxins was carried out by the split-and-pool method. Biological evaluation of the resulting analogs against osteoclast-like multinuclear cells (OCLs) revealed that the N-methyl-alanine residue was crucial to inducing morphological changes in OCLs. In particular, functionalization at the β-position of the proline (Pro) residue was found to be tolerant of the desired biological activity of destruxin E, suggesting that the β-position of the Pro residue should be a promising site for the introduction of a chemical tag toward the preparation of a molecular probe. | |||||||||||
書誌情報 |
en : Chemical & pharmaceutical bulletin 巻 67, 号 10, p. 1023-1029, 発行日 2019-10 |
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ISSN | ||||||||||||
収録物識別子タイプ | ISSN | |||||||||||
収録物識別子 | 0009-2363 | |||||||||||
書誌レコードID | ||||||||||||
収録物識別子タイプ | NCID | |||||||||||
収録物識別子 | AA00602100 | |||||||||||
PubMed番号 | ||||||||||||
識別子タイプ | PMID | |||||||||||
関連識別子 | 31582623 | |||||||||||
DOI | ||||||||||||
識別子タイプ | DOI | |||||||||||
関連識別子 | 10.1248/cpb.c19-00272 | |||||||||||
権利 | ||||||||||||
権利情報 | © 2019 The Pharmaceutical Society of Japan | |||||||||||
著者版フラグ | ||||||||||||
値 | publisher | |||||||||||
出版者 | ||||||||||||
出版者 | Pharmaceutical Society of Japan | |||||||||||
出版者別名 | ||||||||||||
出版者 | 日本薬学会 |