Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophages

Title
Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophages
Authors
장현록모하메드엘가말최혜은최호영이경태오창현
Keywords
Antiinflammatory; Coumarin; Nitric oxide; PGE2; Sulfonate; Tricyclic fused coumarin
Issue Date
2014-01
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 24, NO 2, 571-575
Abstract
The regulations of NO and PGE2 productions are research topics of interest in the field of antiinflammatory drug development. In the present study, a series of tricyclic fused coumarin sulfonate derivatives was synthesized and evaluated for their abilities to inhibit NO and PGE2 productions in LPS-induced RAW 264.7 macrophages. Among all the target compounds, compound 1g possessing p-(trifluoromethyl) phenyl and fused cycloheptane moieties showed the highest inhibitory effects on NO and PGE2 productions. Compound 1g not only inhibited COX-2 activity but also reduced expressions of COX-2 and iNOS. Furthermore, ADME profiling showed that compounds 1g, 1j, 1m, and 1n are estimated to be orally bioavailable.
URI
http://pubs.kist.re.kr/handle/201004/47081
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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