Synthesis and biological evaluation of a beauveriolide analogue library

Kenichiro Nagai, Takayuki Doi, Takafumi Sekiguchi, Ichiji Namatame, Toshiaki Sunazuka, Hiroshi Tomoda, Satoshi Omura, Takashi Takahashi

研究成果: Article査読

40 被引用数 (Scopus)

抄録

Synthesis of beauveriolide III (1b), which is an inhibitor of lipid droplet accumulation in macrophages, was achieved by solid-phase assembly of linear depsipeptide using a 2-chlorotrityl linker followed by solution-phase cyclization. On the basis of this strategy, a combinatorial library of beauveriolide analogues was carried out by radio frequency-encoded combinatorial chemistry. After automated purification using preparative reversed-phase HPLC, the library was tested for inhibitory activity of CE synthesis in macrophages to determine structure-activity relationships of beauveriolides. Among them, we found that diphenyl derivative 7{9,1} is 10 times more potent than 1b.

本文言語English
ページ(範囲)103-109
ページ数7
ジャーナルJournal of Combinatorial Chemistry
8
1
DOI
出版ステータスPublished - 2006 1月 1
外部発表はい

ASJC Scopus subject areas

  • 創薬
  • 有機化学
  • 化学 (全般)
  • 離散数学と組合せ数学

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