Synthesis and antiproliferative activities of quebecol and its analogs |
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| Authors: | 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 |
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| Institution: | 1. Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, Rajasthan, India;2. Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston 02881, RI, USA |
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| Abstract: | 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. The IC50 values for compounds 7c, 7d, and 7f were 85.1 μM, 78.7 μM, and 80.6 μM against MCF-7 cell line, respectively, showing slightly higher antiproliferative activtiy than the synthesized and isolated quebecol with an IC50 value of 104.2 μM against MCF-7. |
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| Keywords: | Antiproliferative Phenolic Quebecol Structure–activity relationship Synthesis |
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