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Sébastien Cardinal, Jabrane Azelmat, Daniel Grenier, Normand Voyer
Herein we report our results on the anti-inflammatory activity of quebecol, a polyphenolic compound discovered in maple syrup. Bioassays demonstrated that quebecol has an anti-inflammatory effect on LPS-induced NF-κB activation and inhibits the secretion of two pro-inflammatory cytokines, IL-6 and TNF-α. We also prepared and tested precursors of quebecol and its derivatives corresponding to its substructures of interest, with the aim to study the structure-activity relationships. Comparing the results obtained for all tested compounds allowed the identification of the main moiety responsible for the anti-inflammatory activity of quebecol...
January 15, 2016: Bioorganic & Medicinal Chemistry Letters
Kasiviswanadharaju Pericherla, Amir Nasrolahi Shirazi, V Kameshwara Rao, Rakesh K Tiwari, Nicholas DaSilva, Kellen T McCaffrey, Yousef A Beni, Antonio González-Sarrías, Navindra P Seeram, Keykavous Parang, Anil Kumar
Simple and efficient synthesis of quebecol and a number of its analogs was accomplished in five steps. The synthesized compounds were evaluated for antiproliferative activities against human cervix adenocarcinoma (HeLa), human ovarian carcinoma (SK-OV-3), human colon carcinoma (HT-29), and human breast adenocarcinoma (MCF-7) cancer cell lines. Among all the compounds, 7c, 7d, 7f, and 8f exhibited antiproliferative activities against four tested cell lines with inhibition over 80% at 75 μM after 72 h, whereas, compound 7b and 7g were more selective towards MCF-7 cell line...
October 1, 2013: Bioorganic & Medicinal Chemistry Letters
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