Discovery of a Highly Tumor-Selective Organometallic Ruthenium(II)-Arene Complex

A ruthenium(II)-arene complex with a perfluoroalkyl-ligand was found to display remarkable selectivity toward cancer cells. IC50 values on several cancer cell lines are in the range of 25-45 mu M, and no cytotoxic effect was observed on nontumorigenic (HEK-293) cells at concentrations up to 500 mu M (the maximum concentration tested). Consequently, this complex was used as the basis for the development of a number of related derivatives, which were screened in cancerous and noncancerous cell lines. The lead compound was then evaluated in vivo for antiangiogenic activity in the CAM model and in a xenografted ovarian carcinoma tumor (A2780) grown on the CAM. A 90% reduction in the tumor growth was observed.


Published in:
Journal Of Medicinal Chemistry, 57, 8, 3546-3558
Year:
2014
Publisher:
Washington, Amer Chemical Soc
ISSN:
0022-2623
Laboratories:




 Record created 2014-05-26, last modified 2018-01-28


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