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Synthesis and PGE2 inhibitory activity of novel diarylheptanoids |
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| Authors: | Richard D. McLane Léon Le Cozannet-Laidin Maxwell S. Boyle Lindsey Lanzillotta Zachary L. Taylor Sarah R. Anthony Michael Tranter Amber J. Onorato |
| Affiliation: | 1. Department of Chemistry, Northern Kentucky University, 1 Nunn Drive, Highland Heights, KY 41099, USA;2. Départment de Measures Physiques, Institut Universitaire de Technologie de Lannion, BP 30219, Rue Edouard Branly, 22302 Lannion Cedex, France;3. Division of Cardiovascular Health and Disease, University of Cincinnati College of Medicine, 231 Albert Sabin Way, Cincinnati, OH 45267, USA |
| Abstract: | Prostaglandin E2 (PGE2) is a lipid mediator of inflammation and its inhibition has become a popular drug target due to its harmful physiological roles. Diarylheptanoids are one class of compounds that have shown successful inhibition of PGE2. This paper reports the synthesis and PGE2 inhibitory activity of a series of analogues of a naturally occurring diarylheptanoid. The most efficacious compounds were examined for dose-dependent PGE2 inhibition. Among several promising compounds, the lead candidate exhibited an IC50 value of 0.56?ng/µL or 1.7?µM with no detectable toxicity at the highest dose of 10?ng/µL. |
| Keywords: | Diarylheptanoids Curcumin Inflammation Cross metathesis |
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