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Electronic State of Sodium trans-[Tetrachloridobis(1H-indazole)ruthenate(III)] (NKP-1339) in Tumor, Liver and Kidney Tissue of a SW480-bearing Mouse

DOI: 10.1038/srep40966 DOI Help

Authors: Amir Blazevic (Universität Wien) , Alfred Hummer (Universität Wien) , Petra Heffeter (Medizinische Universität Wien) , Walter Berger (Medizinische Universität Wien) , Martin Filipits (Medizinische Universität Wien) , Giannantonio Cibin (Diamond Light Source) , Bernhard K. Keppler (Universität Wien) , Annette Rompel (Universität Wien)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Scientific Reports , VOL 7

State: Published (Approved)
Published: January 2017
Diamond Proposal Number(s): 10039

Open Access Open Access

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 RuIIIN2Cl4 to RuIIIClx(N/O)6−x (X = 1 or 2).

Journal Keywords: Biochemistry; Cancer

Subject Areas: Biology and Bio-materials, Chemistry, Medicine


Instruments: B18-Core EXAFS

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srep40966.pdf