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Merck

One pot synthesis and anticancer activity of dimeric phloroglucinols.

Bioorganic & medicinal chemistry letters (2012-02-22)
Siddheshwar K Chauthe, Sandip B Bharate, Giridharan Periyasamy, Amit Khanna, Kamlesh K Bhutani, Prabhu D Mishra, Inder P Singh
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 IC(50) of 5.5 μM in colon cancer cell lines (HCT116).

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