2015年1月
Synthesis and biological evaluation of the [D-MeAla(11)]-epimer of coibamide A
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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- 巻
- 25
- 号
- 2
- 開始ページ
- 302
- 終了ページ
- 306
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.bmcl.2014.11.044
- 出版者・発行元
- PERGAMON-ELSEVIER SCIENCE LTD
Coibamide A is a highly potent antiproliferative cyclic depsipeptide, which was originally isolated from a Panamanian marine cyanobacterium. In this study, the synthesis of coibamide A has been investigated using Fmoc-based solid-phase peptide synthesis followed by the cleavage of the resulting linear peptide from the resin and its subsequent macrolactonization. The peptide sequence of the linear coibamide A precursor was constructed on a solid-support following the optimization of the coupling conditions, where numerous coupling agents were evaluated. The macrocyclization of the resulting linear peptide provided the [D-MeAla(11)]-epimer of coibamide A, which exhibited nanomolar cytotoxic activity towards a number of human cancer cell lines. (C) 2014 Elsevier Ltd. All rights reserved.
- リンク情報
- ID情報
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- DOI : 10.1016/j.bmcl.2014.11.044
- ISSN : 0960-894X
- eISSN : 1464-3405
- PubMed ID : 25488840
- Web of Science ID : WOS:000347901400031