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

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)2597-2601
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number10
DOIs
Publication statusPublished - 2004 May 17

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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