title: New half sandwich Ru(II) coordination compounds for anticancer activity.
abstract: With the aim of expanding the structure-activity relationship investigation, the series of Ru(II) half sandwich coordination compounds of the type [Ru([9]aneS3)(chel)(L)](n+) previously described by us (where [9]aneS3 is the neutral face-capping ligand 1,4,7-trithiacyclononane, chel is a neutral or anonic chelating ligand, L = Cl(-) or dmso-S, n = 0-2) was extended to 1,4,7-triazacyclononane ([9]aneN3). In addition, new neutral N-N, and anionic N-O and O-O chelating ligands, i.e. dach (trans-1,2-diaminocyclohexane), pic(-) (picolinate), and acac(-) (acetylacetonate), were investigated in combination with both [9]aneS3 and [9]aneN3. Overall, ten new half-sandwich complexes were prepared and fully characterized and their chemical behaviour in aqueous solution was established. The single-crystal X-ray structures of eight of them, including the versatile precursor [Ru([9]aneN3)(dmso-S)(2)Cl]Cl (9), were also determined. The results of in vitro antiproliferative tests performed on selected compounds against MDA-MB-231 human mammary carcinoma cells confirmed that, in this series, only compounds that hydrolyse the monodentate ligand at a reasonable rate show moderate activity, provided that the chelate ligand is a hydrogen bond donor.
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, Via L. Giorgieri 1, 34127 Trieste, Italy.
authors.forename: Ioannis
authors.initials: I
authors.lastname: Bratsos
authors.forename: Elisa
authors.initials: E
authors.lastname: Mitri
authors.forename: Francesco
authors.initials: F
authors.lastname: Ravalico
authors.forename: Ennio
authors.initials: E
authors.lastname: Zangrando
authors.forename: Teresa
authors.initials: T
authors.lastname: Gianferrara
authors.forename: Alberta
authors.initials: A
authors.lastname: Bergamo
authors.forename: Enzo
authors.initials: E
authors.lastname: Alessio
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D012428:Ruthenium / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014867:Water / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D014867:Water; D012428:Ruthenium