Combinatorial Synthesis and Biological Evaluation of Destruxins
-
- Yoshida Masahito
- Faculty of Pure and Applied Sciences, University of Tsukuba
この論文をさがす
抄録
<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>
収録刊行物
-
- CHEMICAL & PHARMACEUTICAL BULLETIN
-
CHEMICAL & PHARMACEUTICAL BULLETIN 67 (10), 1023-1029, 2019-10-01
公益社団法人 日本薬学会
- Tweet
詳細情報 詳細情報について
-
- CRID
- 1390845702293679232
-
- NII論文ID
- 130007722022
-
- NII書誌ID
- AA00602100
-
- ISSN
- 13475223
- 00092363
-
- HANDLE
- 2241/00159754
-
- NDL書誌ID
- 029983651
-
- PubMed
- 31582623
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- IRDB
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可