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Preliminary structure-antiangiogenic activity relationships of 4-senecioyloxymethyl-6,7-dimethoxycoumarin.

Abstract：

:Through a systematic modification of the novel angiogenesis inhibitor 4-senecioyloxymethyl-6,7-dimethoxycoumarin (1) we found that a 6,7-dimethoxy moiety is important for bioactivity of 1. Replacement of the lactone functionality in coumarin 1 by an amide decreased its activity. By substitution of the senecioyl chain with various cinnamoyl groups we discovered 6d, bearing a 4-methoxycinnamoyl instead of senecioyl side chain, with inhibitory activity in HUVEC tube formation assay enhanced by one order of magnitude compared to 1. We have also synthesized compound 12, an analogue of 6d, with equipotency and improved water solubility.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Nam NH,Kim Y,You YJ,Hong DH,Kim HM,Ahn BZ

doi

10.1016/s0960-894x(02)00392-x

subject

Has Abstract

pub_date

2002-09-02 00:00:00

pages

2345-8

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960894X0200392X

journal_volume

12

pub_type

杂志文章

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