Discovery of novel osthole derivatives as potential anti-breast cancer treatment.
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.
School of Traditional Chinese Pharmacy, Shanghai University of Traditional Chinese Medicine, Zhangjiang Hi-Tech Park, Shanghai, PR China. youlisha@shutcm.com
Lisha
L
You
Rui
R
An
Xinhong
X
Wang
Yimin
Y
Li
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D031048:Cnidium / Q000737:chemistry; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D005260:Female; D006801:Humans
D000970:Antineoplastic Agents; D003374:Coumarins; C030123:coumarin; C046627:osthol