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One pot synthesis and anticancer activity of dimeric phloroglucinols

  作者 Chauthe, SK; Bharate, SB; Periyasamy, G; Khanna, A; Bhutani, KK; Mishra, PD; Singh, IP  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-6;  页码  2251-2256  
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[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 mu M in colon cancer cell lines (HCT116). (C) 2012 Elsevier Ltd. All rights reserved.

 
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