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

作者：Clavel Catherine M; Paunescu Emilia; Nowak Sliwinska Patrycja; Griffioen Arjan W; Scopelliti Rosario; Dyson Paul J^*

来源：Journal of Medicinal Chemistry, 2014, 57(8): 3546-3558.

DOI：10.1021/jm5002748

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.

• 出版日期2014-4-24