| Item type |
紀要論文(ELS) / Departmental Bulletin Paper(1) |
| 公開日 |
2007-12-01 |
| タイトル |
|
|
タイトル |
ヒストン脱アセチル化酵素阻害物質スピルコスタチンAの合成研究 |
|
言語 |
ja |
| タイトル |
|
|
タイトル |
Synthetic Studies on Spiruchostatin A, a Potent Histone Deacetylase Inhibitor |
|
言語 |
en |
| 言語 |
|
|
言語 |
jpn |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
spiruchostatin A |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
histone deacetylase inhibitor |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
disulfide bond formation |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
macrolactam/macrolactone cyclization |
| 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 |
departmental bulletin paper |
| 著者名 |
瀧澤, 俊也
成田, 紘一
渡邉, 一弘
阿部, 秀樹
加藤, 正
|
| 抄録 |
|
|
内容記述タイプ |
Abstract |
|
内容記述 |
Spiruchostatin A (1), isolated from a culture broth of Pseudomonas sp., has been shown to be a potent histone deacetylase (HDAC) inhibitor. HDAC inhibitors can suppress the growth of human tumor xenografts, this natural product, therefore, is expected to be a promising candidate for novel molecular-targeted anticancer agents. We envisioned that 1 would be synthesized through twofold macrolactam/macrolactone cyclization of the fully elaborated acyclic disulfide 2. The key segments 3 and 4, required for the preparation of the advanced key intermediate 2, were initially synthesized, and the two segments were subsequently subjected to the critical cross S-S coupling reaction to produce the desired key intermediate 11 (synthetically equivalent to 2). Upon deprotection of the N-Boc and the methyl ester groups in 11, the crucial cyclization formation was achieved using PyBOP to provide the desired macrolactam 16, a potential key precursor for 1. Further investigations concerning the transformation of 16 to the target molecule 1 were also described. |
|
言語 |
en |
| 書誌情報 |
ja : 東北薬科大学研究誌
en : Journal of Tohoku Pharmaceutical University
号 54,
p. 33-47,
発行日 2007-12
|
| 雑誌書誌ID |
|
|
収録物識別子タイプ |
NCID |
|
収録物識別子 |
AA1149311X |
KJ00005384866 (1.2 MB)
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