当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and structure-activity relationships of guaiane-type sesquiterpene lactone derivatives with respect to inhibiting NO production in lipopolysaccharide-induced RAW 264.7 macrophages.

Synthesis and structure-activity relationships of guaiane-type sesquiterpene lactone derivatives with respect to inhibiting NO production in lipopolysaccharide-induced RAW 264.7 macrophages.

Abstract：

:A guaiane framework was scaffolded by photochemical rearrangement reactions using α-santonin 1 as a starting material. Then, using a series of reactions, we synthesized the guaiane-type sesquiterpene lactone 5 in high yield. The inhibitory activities of compound 5 and of a series of derivatives on nitric oxide (NO) release were evaluated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Compounds 6g, 7h, 7i, 7k and 8g, exhibited significant inhibitory effects on NO production, with IC50 values of 14.8, 22.3, 18.3, 17.4 and 7.0 μM, respectively. Their cytotoxicities were also estimated using an MTT assay. The structure-activity relationships of these compounds were also discussed.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Chen H,Chen BY,Liu CT,Zhao Z,Shao WH,Yuan H,Bi KJ,Liu JY,Sun QY,Zhang WD

doi

10.1016/j.ejmech.2014.06.043

subject

Has Abstract

pub_date

2014-08-18 00:00:00

pages

307-16

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00572-8

journal_volume

83

pub_type

杂志文章

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