Discovery of novel osthole derivatives as potential anti-breast cancer treatment.

Bioorg Med Chem Lett

School of Traditional Chinese Pharmacy, Shanghai University of Traditional Chinese Medicine, Zhangjiang Hi-Tech Park, Shanghai, PR China.

Published: December 2010

Osthole, an ingredient of Traditional Chinese Medicine (TCM) from natural product Cnidium monnieri (L.) Cusson, was used as a lead compound for structural modification. A series of osthole derivatives bearing aryl substituents at 3-position of coumarin, has been prepared and evaluated for their growth inhibitory activity against human breast cancer cell lines MCF-7 and MDA-MB-231. Interestingly, some derivatives exhibited good inhibition, among them compound 8e was found to be the most potent compound with IC(50) values of 0.24 μM, 0.31 μM against MCF-7 and MDA-MB-231, respectively, which was improved more than 100-folds compared with its parent compound osthole.

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http://dx.doi.org/10.1016/j.bmcl.2010.10.027DOI Listing

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