title: Antitumor activity of new hydridotris(pyrazolyl)borate ruthenium(II) complexes containing the phosphanes PTA and 1-CH3-PTA.
abstract: The synthesis and full characterization of new half-sandwich ruthenium(II) complexes containing κ(3)(N,N,N)-hydridotris(pyrazolyl)borate (κ(3)(N,N,N)-Tp) and the water-soluble phosphanes 1,3,5-triaza-7-phosphatricyclo[3.3.1.1(3,7)]decane (PTA) and 1-methyl-3,5-diaza-1-azonia-7-phosphatricyclo[3.3.1.1(3,7)]decane (1-CH(3)-PTA) has been explored. Single crystal X-ray diffraction analysis for complex [RuCl{κ(3)(N,N,N)-Tp}(PMe(2)Ph)(1-CH(3)-PTA)][CF(3)SO(3)]·2NCMe is also reported. DNA binding properties of the ruthenium complexes have been evaluated by mobility shift assay and MALDI-TOF mass spectrometry. The in vitro antitumor activity of these compounds was assessed by examining their ability to inhibit cell proliferation in a number of human cancer cell lines (NCI-H460, SF-268, MCF-7) and non-tumor human umbilical vein endothelial cells (HUVEC). Some of these new compounds show promising cytotoxic activity with IC(50) values in the low micromolar range, and display differential effects on cancer and normal cell growth.
authors.affiliation: Departamento de Química Orgánica e Inorgánica, Instituto de Química Organometálica Enrique Moles (Unidad Asociada al C.S.I.C.). Universidad de Oviedo, 33006, Oviedo, Spain.
authors.forename: Almudena
authors.initials: A
authors.lastname: García-Fernández
authors.forename: Josefina
authors.initials: J
authors.lastname: Díez
authors.forename: Angel
authors.initials: A
authors.lastname: Manteca
authors.forename: Jesús
authors.initials: J
authors.lastname: Sánchez
authors.forename: Rósula
authors.initials: R
authors.lastname: García-Navas
authors.forename: Beatriz G
authors.initials: BG
authors.lastname: Sierra
authors.forename: Faustino
authors.initials: F
authors.lastname: Mollinedo
authors.forename: M Pilar
authors.initials: MP
authors.lastname: Gamasa
authors.forename: Elena
authors.initials: E
authors.lastname: Lastra
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D001483:Base Sequence; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA / Q000235:genetics / Q000378:metabolism; D004563:Electrochemistry; D006801:Humans; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D010720:Phosphines / Q000737:chemistry*; D011720:Pyrazoles / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D010720:Phosphines; D011720:Pyrazoles; C031280:pyrazole; D012428:Ruthenium; D004247:DNA; C044646:phosphine