2019年
Combinatorial Synthesis and Biological Evaluation of Destruxins
CHEMICAL & PHARMACEUTICAL BULLETIN
- 巻
- 67
- 号
- 10
- 開始ページ
- 1023
- 終了ページ
- 1029
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1248/cpb.c19-00272
- 出版者・発行元
- 公益社団法人 日本薬学会
<p>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.</p>
- ID情報
-
- DOI : 10.1248/cpb.c19-00272
- ISSN : 0009-2363