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Article Abstract

Herein, we describe the synthesis and evaluation of anti-inflammatory activities of new curcumin derivatives. The thirteen curcumin derivatives were synthesized by Steglich esterification on one or both of the phenolic rings of curcumin with the aim of providing improved anti-inflammatory activity. Monofunctionalized compounds showed better bioactivity than the difunctionalized derivatives in terms of inhibiting IL-6 production, and known compound presented the highest activity. Additionally, this compound showed strong activity against PGE. Structure-activity relationship studies were carried out for both IL-6 and PGE, and it was found that the activity of this series of compounds increases when a free hydroxyl group or aromatic ligands are present on the curcumin ring and a linker moiety is absent. Compound remained the highest activity in modulating IL-6 production and showed strong activity against PGE synthesis.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9966181PMC
http://dx.doi.org/10.3390/ijms24043691DOI Listing

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