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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Murakami N,Tamura S,Koyama K,Sugimoto M,Maekawa R,Kobayashi M

doi

10.1016/j.bmcl.2004.02.080

subject

Has Abstract

pub_date

2004-05-17 00:00:00

pages

2597-601

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960894X04002975

journal_volume

14

pub_type

杂志文章

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