title: Synthesis, characterization, DNA interactions and antiproliferative activity on glioblastoma of iminopyridine platinum(II) chelate complexes.
abstract: A series of iminopyridine platinum chelate compounds has been prepared and characterized by NMR spectroscopy and single-crystal X-ray diffraction. The complexes were evaluated in C6 tumoral cells as an in vitro model for glioblastoma multiforme. The DNA-binding properties of these complexes were studied by UV-Vis absorption and fluorescence spectroscopy and Density Functional Theory calculations were performed in an effort to rationalize the observed properties at the molecular level. The most promising drug candidate displayed a similar potency in inducing cell death to the clinically used reference compound and showed significant inhibition of glioblastoma cell proliferation. Moreover, this compound had a safer profile than cisplatin on non-tumoral cells.
authors.affiliation: Unidad Asociada Neurodeath CSIC-UCLM, Departamento de Ciencias Médicas, Facultad de Farmacia, Universidad de Castilla-La Mancha, Campus Universitario de Albacete, 02071 Albacete, Spain; CIBERNED, Instituto de Salud Carlos III, Madrid, Spain.
authors.forename: Inmaculada
authors.initials: I
authors.lastname: Posadas
authors.affiliation: Departamento de Química Inorgánica, Orgánica y Bioquímica, Universidad de Castilla-La Mancha, Facultad de Farmacia, Campus Universitario de Albacete, 02071 Albacete, Spain. Electronic address: carlos.amoreno@uclm.es.
authors.forename: Carlos
authors.initials: C
authors.lastname: Alonso-Moreno
authors.affiliation: Departamento de Química-Física, Universidad de Castilla-La Mancha, Facultad de Farmacia, Campus Universitario de Albacete, 02071 Albacete, Spain.
authors.forename: Iván
authors.initials: I
authors.lastname: Bravo
authors.affiliation: Departamento de Química Inorgánica, Orgánica y Bioquímica, Universidad de Castilla-La Mancha, Facultad de Ciencias y Tecnologías Químicas, Campus Universitario de Ciudad Real, 13071 Ciudad Real, Spain.
authors.forename: Fernando
authors.initials: F
authors.lastname: Carrillo-Hermosilla
authors.affiliation: Departamento de Química-Física, Universidad de Castilla-La Mancha, Facultad de Farmacia, Campus Universitario de Albacete, 02071 Albacete, Spain.
authors.forename: Andrés
authors.initials: A
authors.lastname: Garzón
authors.affiliation: Departamento de Química-Física, Universidad de Castilla-La Mancha, Facultad de Farmacia, Campus Universitario de Albacete, 02071 Albacete, Spain.
authors.forename: Noemí
authors.initials: N
authors.lastname: Villaseca
authors.affiliation: Departamento de Química Inorgánica, Orgánica y Bioquímica, Universidad de Castilla-La Mancha, Facultad de Ciencias y Tecnologías Químicas, Campus Universitario de Ciudad Real, 13071 Ciudad Real, Spain.
authors.forename: Isabel
authors.initials: I
authors.lastname: López-Solera
authors.affiliation: Departamento de Química-Física, Universidad de Castilla-La Mancha, Facultad de Ciencias y Tecnologías Químicas, Campus Universitario de Ciudad Real, 13071 Ciudad Real, Spain; Departamento de Química Inorgánica, Orgánica y Bioquímica, Universidad de Castilla-La Mancha, Facultad de Ciencias y Tecnologías Químicas, Campus Universitario de Ciudad Real, 13071 Ciudad Real, Spain.
authors.forename: José
authors.initials: J
authors.lastname: Albaladejo
authors.affiliation: Unidad Asociada Neurodeath CSIC-UCLM, Departamento de Ciencias Médicas, Facultad de Medicina, Universidad de Castilla-La Mancha, Campus Universitario de Albacete, 02071 Albacete, Spain; CIBERNED, Instituto de Salud Carlos III, Madrid, Spain.
authors.forename: Valentín
authors.initials: V
authors.lastname: Ceña
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004247:DNA / Q000737:chemistry*; D005909:Glioblastoma / Q000188:drug therapy*; D007097:Imines / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D010984:Platinum / Q000737:chemistry* / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D051381:Rats
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D007097:Imines; D011725:Pyridines; D010984:Platinum; D004247:DNA
keywords: Cisplatin derivatives; DNA-binding; Glioblastoma