Structure-activity relationship study on 13-deoxytedanolide, a highly antitumor macrolide from the marine sponge Mycale adhaerens

Shinichi Nishimura, Shigeki Matsunaga, Satoru Yoshida, Yoichi Nakao, Hiroshi Hirota, Nobuhiro Fusetani

研究成果: Article査読

31 被引用数 (Scopus)

抄録

Structure-activity relationship of 13-deoxytedanolide showed that the southern and northern hemispheres play independent roles to exhibit potent biological activity. To obtain information of structure-activity relationships (SARs) of 13-deoxytedanolide, its chemical transformation has been carried out, targeting on such functional groups as an epoxide, hydroxyls, ketones, and olefins. A total of 10 derivatives have been prepared and their cytotoxicity against P388 murine leukemia cells and inhibitory activity of polypeptide elongation in yeast cell lysate provided some important SARs; the southern hemisphere comprises the pharmacophore, while the epoxide-bearing side chain is essential for the activity.

本文言語English
ページ(範囲)455-462
ページ数8
ジャーナルBioorganic and Medicinal Chemistry
13
2
DOI
出版ステータスPublished - 2005 1 17
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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