title: New mononuclear and homodinuclear Pt(ii) complexes with heterocyclic nitrogen chelates: synthesis, characterization, intercalating ability and in vitro cytotoxic activity evaluation.
abstract: A series of new mononuclear and dinuclear platinum(ii) compounds based on two bipyridyl systems, linked by an alkyl chain {1,2-bis[4-(4'-methyl-2,2'-bipyridinyl)]ethane, L2, (a), and 1,6-bis[4-(4'-methyl-2,2'-bipyridinyl)]hexane, L6, (b)} have been synthesized and characterized by IR and multinuclear and multidimensional NMR spectroscopy. The coordination sphere of the complexes, designed to give intercalating and/or covalent interactions with DNA, is completed only by exchangeable (Cl(-), I(-) or H(2)O) and/or not leaving (chelate ethylenediamine, en) saturating ligands. Quenching of the DNA-ethidium fluorescence was performed in order to verify the intercalating capability of the water soluble compounds. Furthermore, the in vitro cytotoxicity of all water soluble complexes has been assessed with respect to cisplatin on platinum-sensitive human endometrium (HeLa) and platinum-resistant human breast (MCF-7) cancer cell lines.
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche ed Ambientali, Università del Salento, prov.le Lecce/Monteroni, I-73100 Lecce, Italy.
authors.forename: Sandra A
authors.initials: SA
authors.lastname: De Pascali
authors.forename: Danilo
authors.initials: D
authors.lastname: Migoni
authors.forename: Paride
authors.initials: P
authors.lastname: Papadia
authors.forename: Alessandro
authors.initials: A
authors.lastname: Romano
authors.forename: Santo
authors.initials: S
authors.lastname: Marsigliante
authors.forename: Aymeric
authors.initials: A
authors.lastname: Pellissier
authors.forename: Sylvie
authors.initials: S
authors.lastname: Chardon-Noblat
authors.forename: Antonella
authors.initials: A
authors.lastname: Ciccarese
authors.forename: Francesco P
authors.initials: FP
authors.lastname: Fanizzi
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D006801:Humans; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009584:Nitrogen / Q000737:chemistry*; D017671:Platinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*
chemical_list: D002614:Chelating Agents; D006571:Heterocyclic Compounds; D008024:Ligands; D017671:Platinum Compounds; D009584:Nitrogen