title: Ruthenium (II) nitrofurylsemicarbazone complexes: new DNA binding agents.
abstract: Complexes of the type [Ru(II)Cl(2)(DMSO)(2)L], where L are 5-nitrofurylsemicarbazone derivatives, were prepared in an effort to combine the potential anti-tumor activity of the metal and the free ligands. The new complexes are excellent DNA binding agents for calf thymus DNA. So, their in vitro anti-tumor activity was tested in cellular models and the complexes were found to be non-cytotoxic on the tumor cell lines assayed, neither in aerobic conditions nor in the bio-reductive assay performed. Redox behavior, lipophilicity and stability were studied in order to explain the lack of cellular cytotoxic effects. The complexes resulted 10-100 times more hydrophilic than the parent ligands thus the bio-activity of these compounds would be compromised by their inadequate lipophilic properties.
authors.affiliation: Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
authors.forename: Eliana
authors.initials: E
authors.lastname: Cabrera
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
authors.forename: Dinorah
authors.initials: D
authors.lastname: Gambino
authors.forename: Pabla
authors.initials: P
authors.lastname: Noblia
authors.forename: Lucía
authors.initials: L
authors.lastname: Otero
authors.forename: Beatriz
authors.initials: B
authors.lastname: Parajón-Costa
authors.forename: Atilio
authors.initials: A
authors.lastname: Anzellotti
authors.forename: Roberto
authors.initials: R
authors.lastname: Sánchez-Delgado
authors.forename: Amaia
authors.initials: A
authors.lastname: Azqueta
authors.forename: Adela
authors.initials: A
authors.lastname: López de Ceráin
authors.forename: Antonio
authors.initials: A
authors.lastname: Monge
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D004247:DNA / Q000187:drug effects* / Q000378:metabolism; D018736:DNA Adducts / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D009593:Nitroimidazoles / Q000737:chemistry; D009942:Organometallic Compounds / Q000737:chemistry / Q000494:pharmacology; D010084:Oxidation-Reduction; D012428:Ruthenium / Q000737:chemistry*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D018736:DNA Adducts; D009593:Nitroimidazoles; D009942:Organometallic Compounds; D012428:Ruthenium; D004247:DNA; C427203:calf thymus DNA