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Synthesis, in vitro inhibitory activity towards COX-2 and haemolytic activity of derivatives of esculentoside A.

Abstract：

:Esculentoside A (EsA) has been reported to possess anti-inflammatory activity and selective inhibitory activity towards cyclooxygenase-2. A series of derivatives of EsA were synthesized by converting the C-28 carboxylic acid group into amides. The haemolytic activity and inhibitory activity towards cyclooxygenase-2 were evaluated in vitro. The SAR study of the derivatives was conducted and showed that introducing aromatic ring to EsA greatly enhanced its biological activity. Compound 23 showed higher inhibitory activity than Celecoxib and EsA, but lower haemolytic toxicity than EsA.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wu F,Yi Y,Sun P,Zhang D

doi

10.1016/j.bmcl.2007.10.006

subject

Has Abstract

pub_date

2007-12-01 00:00:00

pages

6430-3

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01175-4

journal_volume

17

pub_type

杂志文章

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