One pot synthesis and anticancer activity of dimeric phloroglucinols

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• 作者：Siddheshwar K. Chauthe^a ; Sandip B. Bharate^a ; Giridharan Periyasamy^b ; Amit Khanna^b ; Kamlesh K. Bhutani^a ; Prabhu D. Mishra^b ; Inder P. Singh^a ; ^{ipsingh@niper.ac.in} ; ^{ipsingh67@yahoo.com}
• 关键词：Phloroglucinol ; Anticancer ; Dimeric ; Cytotoxic ; 2 ; 4-Diacetyl phloroglucinol
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March, 2012
• 卷：22
• 期：6
• 页码：2251-2256
• 文件大小：360 K

摘要

A series of dimeric phloroglucinol compounds were synthesized in a single step using commercially available phloroglucinol and methanesulfonic acid. Based on the reported anticancer activity of plant derived dimeric phloroglucinols, these synthesized compounds were evaluated for their in vitro anti-proliferative activities against various cancer cell lines. Several compounds demonstrated in vitro cytotoxic effects across a wide array of tumor cell types. The compound 29 with pyridin-3-yl group on linker methylene and two diisovaleryl phloroglucinol moieties was found to be the most active in all the five cancer cell lines having a low IC₅₀ of 5.5 渭M in colon cancer cell lines (HCT116).