X-ray Absorption Near Edge Structure Spectroscopy to Resolve the in Vivo Chemistry of the Redox-Active Indazoliumtrans-[Tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019)

• DOI: 10.1021/jm301648f
• Publication Date: 2013-01-03T13:09:48Z
• Authors: Alfred A. Hummer; Petra Heffeter; Walter Berger; Martin Filipits; David Batchelor; Gabriel E. Büchel; Michael A. Jakupec; Bernhard K. Keppler; Annette Rompel
• Keywords: Indazole

Indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (1, KP1019) and its analogue sodium (2, KP1339) are promising redox-active anticancer drug candidates that were investigated with X-ray absorption near edge structure spectroscopy. The analysis was based on the concept of coordination charge ruthenium model compounds representing possible coordinations oxidation states in vivo. 1 citrate saline buffer (pH 3.5) carbonate 7.4) at 37 °C for different time intervals. Interaction studies glutathione apo-transferrin undertaken, 2 tumor tissues studied too. most likely compound under above mentioned conditions assigned. Microprobe fluorescence thin sections showed strong penetration into tissue, highest concentrations blood vessels regions tissue samples.