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Bioorg Med Chem Lett. 2010 Dec 15;20(24):7426-8. doi: 10.1016/j.bmcl.2010.10.027. Epub 2010 Nov 2.

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

Author information

1
School of Traditional Chinese Pharmacy, Shanghai University of Traditional Chinese Medicine, Zhangjiang Hi-Tech Park, Shanghai, PR China. youlisha@shutcm.com

Abstract

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.

PMID:
21051232
DOI:
10.1016/j.bmcl.2010.10.027
[Indexed for MEDLINE]

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