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 mu M 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 mu M, 78.7 mu M, and 80.6 mu M against MCF-7 cell line, respectively, showing slightly higher antiproliferative activtiy than the synthesized and isolated quebecol with an IC50 value of 104.2 mu M against MCF-7.
Pericherla, Kasiviswanadharaju, Amir Nasrolahi Shirazi, V. Kameshwara Rao, Rakesh K. Tiwari, Nicholas DaSilva, Kellen T. McCaffrey, Yousef A. Beni et al. "Synthesis and antiproliferative activities of quebecol and its analogs." Bioorganic & medicinal chemistry letters 23, no. 19 (2013): 5329-5331.
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