title: Ruthenium(II/III)-based compounds with encouraging antiproliferative activity against non-small-cell lung cancer.
abstract: Hereby we present the synthesis of several ruthenium(II) and ruthenium(III) dithiocarbamato complexes. Proceeding from the Na[trans-Ru(III)(dmso)(2)Cl(4)] (2) and cis-[Ru(II)(dmso)(4)Cl(2)] (3) precursors, the diamagnetic, mixed-ligand [Ru(II)L(2)(dmso)(2)] complexes 4 and 5, the paramagnetic, neutral [Ru(III)L(3)] monomers 6 and 7, the antiferromagnetically coupled ionic α-[Ru(III)(2)L(5)]Cl complexes 8 and 9 as well as the β-[Ru(III)(2)L(5)]Cl dinuclear species 10 and 11 (L = dimethyl- (DMDT) and pyrrolidinedithiocarbamate (PDT)) were obtained. All the compounds were fully characterised by elemental analysis as well as (1)H NMR and FTIR spectroscopy. Moreover, for the first time the crystal structures of the dinuclear β-[Ru(III)(2)(dmdt)(5)]BF(4)⋅CHCl(3)⋅CH(3)CN and of the novel [Ru(II)L(2)(dmso)(2)] complexes were also determined and discussed. For both the mono- and dinuclear Ru(II) and Ru(III) complexes the central metal atoms assume a distorted octahedral geometry. Furthermore, in vitro cytotoxicity of the complexes has been evaluated on non-small-cell lung cancer (NSCLC) NCI-H1975 cells. All the mono- and dinuclear Ru(III) dithiocarbamato compounds (i.e., complexes 6-10) show interesting cytotoxic activity, up to one order of magnitude higher with respect to cisplatin. Otherwise, no significant antiproliferative effect for either the precursors 2 and 3 or the Ru(II) complexes 4 and 5 has been observed.
authors.affiliation: Department of Chemical Sciences, University of Padova, Via Marzolo 1, 35131 Padova, Italy.
authors.forename: Eszter M
authors.initials: EM
authors.lastname: Nagy
authors.forename: Andrea
authors.initials: A
authors.lastname: Pettenuzzo
authors.forename: Giulia
authors.initials: G
authors.lastname: Boscutti
authors.forename: Luciano
authors.initials: L
authors.lastname: Marchiò
authors.forename: Lisa
authors.initials: L
authors.lastname: Dalla Via
authors.forename: Dolores
authors.initials: D
authors.lastname: Fregona
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D018360:Crystallography, X-Ray; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy; D008968:Molecular Conformation; D009942:Organometallic Compounds / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D012428:Ruthenium / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D009942:Organometallic Compounds; C038741:dichlorotetrakis(dimethyl sulfoxide)ruthenium II; D012428:Ruthenium