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

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.
AuthorsNobutoshi Murakami, Satoru Tamura, Kouhei Koyama, Masanori Sugimoto, Ryuji Maekawa, Motomasa Kobayashi
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 14 Issue 10 Pg. 2597-601 (May 17 2004) ISSN: 0960-894X [Print] England
PMID15109660 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Cytotoxins
  • Depsipeptides
  • arenastatin A
Topics
  • Animals
  • Antineoplastic Agents (administration & dosage, chemical synthesis)
  • Carcinoma, Lewis Lung (drug therapy)
  • Cytotoxins
  • Depsipeptides (administration & dosage, chemical synthesis, therapeutic use)
  • Dose-Response Relationship, Drug
  • Drug Stability
  • Mice
  • Molecular Conformation
  • Porifera (chemistry)
  • Structure-Activity Relationship
  • Treatment Outcome

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