New analogue of arenastatin A, a potent cytotoxic spongean depsipeptide, with anti-tumor activity

Nobutoshi Murakami, Satoru Tamura, Kouhei Koyama, Masanori Sugimoto, Ryuji Maekawa, Motomasa Kobayashi

研究成果: Article査読

9 被引用数 (Scopus)

抄録

Two analogues possessing steric hindered substituents on C-15 of arenastatin A (1), a potent cytotoxic spongean depsipeptide, were synthesized and shown to enhance stability in mouse serum. Notably, 15-tert-butylanalogue (6) with higher cytotoxicity exhibited in vivo anti-tumor activity through iv administration different from 1. Additionally, conformation analysis among the two analogues and arenastatin A (1) indicated that the torsion angle from C-14 to C-20 is a conclusive factor for the potent cytotoxicity of 1.

本文言語English
ページ(範囲)2597-2601
ページ数5
ジャーナルBioorganic and Medicinal Chemistry Letters
14
10
DOI
出版ステータスPublished - 2004 5 17

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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