title: Synthesis, Structure, and Anticancer Activity of Arene-Ruthenium(II) Complexes with Acylpyrazolones Bearing Aliphatic Groups in the Acyl Moiety.
abstract: A series of neutral ruthenium(II) arene complexes [(arene)Ru(QR)Cl] (arene = p-cymene (cym) or hexamethylbenzene (hmb)) containing 4-acyl-5-pyrazolonate QRligands with different electronic and steric substituents (R = 4-cyclohexyl, 4-stearoyl, or 4-adamantyl) and related ionic complexes [(arene)Ru(QR)(PTA)][PF6] (PTA = 1,3,5-triaza-7-phosphaadamantane) were synthesized and characterized by spectroscopy (IR, UV-vis, ESI-MS, and1H and13C NMR), elemental analysis, X-ray crystallography, and density functional theory studies. The cytotoxicity of the proligands and metal complexes was evaluated in vitro against human ovarian carcinoma cells (A2780 and A2780cisR), as well as against nontumorous human embryonic kidney (HEK293) cells. In general the cationic PTA-containing complexes are more cytotoxic than their neutral precursors with a chloride ligand in place of the PTA. Moreover, the complexes do not show cross-resistance and are essentially equally cytotoxic to both the A2780 and A2780cisR cell lines, although they only show limited selectivity toward the cancer cell lines.
authors.forename: Jessica
authors.initials: J
authors.lastname: Palmucci
authors.forename: Fabio
authors.initials: F
authors.lastname: Marchetti
authors.forename: Riccardo
authors.initials: R
authors.lastname: Pettinari
authors.forename: Claudio
authors.initials: C
authors.lastname: Pettinari
authors.affiliation: Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne , 1015 Lausanne, Switzerland.
authors.forename: Rosario
authors.initials: R
authors.lastname: Scopelliti
authors.affiliation: Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne , 1015 Lausanne, Switzerland.
authors.forename: Tina
authors.initials: T
authors.lastname: Riedel
authors.affiliation: Institute of Chemistry, University of Neuchatel , Ave de Bellevaux 51, Neuchatel, CH 2000, Switzerland.
authors.forename: Bruno
authors.initials: B
authors.lastname: Therrien
authors.affiliation: Departamento de Química Inorgánica, Facultad de Química, Universidad de Sevilla , Aptdo 1203, 41071 Sevilla, Spain.
authors.forename: Agustin
authors.initials: A
authors.lastname: Galindo
authors.affiliation: Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne , 1015 Lausanne, Switzerland.
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Dyson
mesh_terms: D002460:Cell Line; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006838:Hydrocarbons / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D011720:Pyrazoles / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship
chemical_list: D056831:Coordination Complexes; D006838:Hydrocarbons; D011720:Pyrazoles; D012428:Ruthenium