title: Electronic State of Sodium trans-[Tetrachloridobis(1H-indazole)ruthenate(III)] (NKP-1339) in Tumor, Liver and Kidney Tissue of a SW480-bearing Mouse.
abstract: Ruthenium complexes are promising candidates for anticancer agents, especially NKP-1339 (sodium trans-[tetrachloridobis(1H-indazole)ruthenate(III)]), which is on the edge to clinical applications. The anticancer mechanism seems to be tightly linked to the redox chemistry but despite progress in human clinical trials the in vivo Ru oxidation state and the coordination of Ru remains unclear. The Ru-based anticancer drug NKP-1339 was studied applying XANES (Cl K- and Ru L2,3-edges) in tumor, kidney and liver tissue of a SW480 bearing mouse. Based on coordination charge and 3D XANES plots containing a series of model compounds as well as pre-edge analysis of the ligand Cl K-edge it is suggested that NKP-1339 remains in its +III oxidation state after 24 hours and at least one of the four chlorido ligands remain covalently bound to the Ru ion showing a biotransformation from RuIIIN2Cl4to RuIIIClx(N/O)6-x(X = 1 or 2).
authors.affiliation: Universität Wien, Fakultät für Chemie, Institut für Biophysikalische Chemie, Althanstraße 14, 1090 Wien, Austria.
authors.forename: Amir
authors.initials: A
authors.lastname: Blazevic
authors.affiliation: Universität Wien, Fakultät für Chemie, Institut für Biophysikalische Chemie, Althanstraße 14, 1090 Wien, Austria.
authors.forename: Alfred A
authors.initials: AA
authors.lastname: Hummer
authors.affiliation: Medizinische Universität Wien, Institut für Krebsforschung, "Comprehensive Cancer Center" und Forschungsplattform "Translational Cancer Therapy Research", Borschkegasse 8a, 1090 Wien, Austria.
authors.forename: Petra
authors.initials: P
authors.lastname: Heffeter
authors.affiliation: Medizinische Universität Wien, Institut für Krebsforschung, "Comprehensive Cancer Center" und Forschungsplattform "Translational Cancer Therapy Research", Borschkegasse 8a, 1090 Wien, Austria.
authors.forename: Walter
authors.initials: W
authors.lastname: Berger
authors.affiliation: Medizinische Universität Wien, Institut für Krebsforschung, "Comprehensive Cancer Center" und Forschungsplattform "Translational Cancer Therapy Research", Borschkegasse 8a, 1090 Wien, Austria.
authors.forename: Martin
authors.initials: M
authors.lastname: Filipits
authors.affiliation: Diamond Light Source, Didcot, OX11 0DE, United Kingdom.
authors.forename: Giannantonio
authors.initials: G
authors.lastname: Cibin
authors.affiliation: Universität Wien, Fakultät für Chemie, Institut für Anorganische Chemie und Forschungsplattform "Translational Cancer Therapy Research", Währinger Straße 42, 1090 Wien, Austria.
authors.forename: Bernhard K
authors.initials: BK
authors.lastname: Keppler
authors.affiliation: Universität Wien, Fakultät für Chemie, Institut für Biophysikalische Chemie, Althanstraße 14, 1090 Wien, Austria.
authors.forename: Annette
authors.initials: A
authors.lastname: Rompel
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000032:analysis; D003110:Colonic Neoplasms / Q000188:drug therapy*; D056831:Coordination Complexes / Q000008:administration & dosage* / Q000032:analysis; D004195:Disease Models, Animal; D006801:Humans; D007668:Kidney / Q000737:chemistry*; D008099:Liver / Q000737:chemistry*; D051379:Mice; D009369:Neoplasms / Q000737:chemistry*; D056928:X-Ray Absorption Spectroscopy
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; C000600110:NKP-1339