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Synthesis of 15,20-triamide analogue with polar substituent on the phenyl ring of arenastatin A, an extremely potent cytotoxic spongean depsipeptide.

Abstract：

:In order to increase metabolic stability and water solubility of arenastatin A, an extremely potent cytotoxic depsipeptide from the Okinawan marine sponge of Dysidea arenaria, several 15,20-triamide analogues with a polar substituent on the phenyl ring were synthesized. The 15,20-triamide analogues with a polar substituent (24, 30, and 31) showed increased solubility to MeOH and stronger cytotoxicity against KB cells in comparison with the parental 15,20-triamide analogue (2). Furthermore, the diethylamine analogue (30) exhibited in vivo anti-tumor activity against subcutaneously implanted murine sarcoma.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kotoku N,Kato T,Narumi F,Ohtani E,Kamada S,Aoki S,Okada N,Nakagawa S,Kobayashi M

doi

10.1016/j.bmc.2006.07.019

subject

Has Abstract

pub_date

2006-11-15 00:00:00

pages

7446-57

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(06)00575-X

journal_volume

14

pub_type

杂志文章

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