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

Abstract

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 μM, and no cytotoxic effect was observed on nontumorigenic (HEK-293) cells at concentrations up to 500 μM (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