Synthesis and antiproliferative activities of quebecol and its analogs

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• 作者：Kasiviswanadharaju Pericherla ; Amir Nasrolahi Shirazi ; V. Kameshwara Rao ; Rakesh K. Tiwari ; Nicholas DaSilva ; Kellen T. McCaffrey ; Yousef A. Beni ; Antonio Gonz¨¢lez-Sarr¨ªas ; Navindra P. Seeram ; Keykavous Parang ; Anil Kumar
• 关键词：Antiproliferative ; Phenolic ; Quebecol ; Structure&ndash ; activity relationship ; Synthesis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 October, 2013
• 年：2013
• 卷：23
• 期：19
• 页码：5329-5331
• 全文大小：486 K

文摘

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 ¦ÌM 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 ¦ÌM, 78.7 ¦ÌM, and 80.6 ¦ÌM against MCF-7 cell line, respectively, showing slightly higher antiproliferative activtiy than the synthesized and isolated quebecol with an IC₅₀ value of 104.2 ¦ÌM against MCF-7.