title: 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.
authors.affiliation: Institut des Sciences et Ingénierie Chimiques , Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.
authors.forename: Catherine M
authors.initials: CM
authors.lastname: Clavel
authors.forename: Emilia
authors.initials: E
authors.lastname: Păunescu
authors.forename: Patrycja
authors.initials: P
authors.lastname: Nowak-Sliwinska
authors.forename: Arjan W
authors.initials: AW
authors.lastname: Griffioen
authors.forename: Rosario
authors.initials: R
authors.lastname: Scopelliti
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Dyson
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002642:Chick Embryo; D055808:Drug Discovery; D057809:HEK293 Cells; D006801:Humans; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D017975:Ruthenium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D017975:Ruthenium Compounds