Design and synthesis of 4-O-methylhonokiol analogs as inhibitors of cyclooxygenase-2 (COX-2) and PGF 1 production

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Title
Design and synthesis of 4-O-methylhonokiol analogs as inhibitors of cyclooxygenase-2 (COX-2) and PGF 1 production
Author(s)
B Lee; J H Kwak; S W Huang; J Y Jang; S Lim; Young Shin Kwak; K Lee; H S Kim; S B Han; J T Hong; H Lee; S Song; S Y Seo; J K Jung
Bibliographic Citation
Bioorganic & Medicinal Chemistry, vol. 20, no. 9, pp. 2860-2868
Publication Year
2012
Abstract
A series of novel 4-O-methylhonokiol analogs were synthesized in light of revealing structure-activity relationship for inhibitory effect of COX-2 enzyme. The key strategy of the molecular design was oriented towards modification of the potential metabolic soft spots (e.g., phenol and olefin) or by altering the polar surface area via incorporating heterocycles such as isoxazole and triazole. Most of all exhibited the inhibitory effects on COX-2 and PGF 1 production but not macrophage NO production. Especially, aryl carbamates 10 and 11 exhibited more potent inhibitory activity against COX-2 and PGF 1 production.
Keyword
4-O-MethylhonokiolAryl carbamateCyclooxygenase-2 (COX-2)IsoxazoleTriazole
ISSN
0968-0896
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmc.2012.03.028
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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