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Hydrolysis study of the bifunctional antitumour compound RAPTA-C, [Ru(eta6-p-cymene)Cl2(pta)
Authors:Scolaro Claudine  Hartinger Christian G  Allardyce Claire S  Keppler Bernhard K  Dyson Paul J
Affiliation:a Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne (EPFL), 1015 Lausanne, Switzerland
b University of Vienna, Institute of Inorganic Chemistry, Währinger Straße 42, A-1090 Vienna, Austria
Abstract:The hydrolysis of [Ru(η6-p-cymene)Cl2(PTA)] (PTA = 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decanephosphine; RAPTA-C) was studied using UV-visible (UV-vis) spectrophotometry and NMR spectroscopy. In analogy to in silico studies, [Ru(η6-p-cymene)Cl(H2O)(PTA)]+ was found to be the most abundant hydrolysis product, although the dihydrolysed species [Ru(η6-p-cymene)(OH)(H2O)(PTA)]+ and the dichloro compound are present. Rate constants for the different aquation and anation steps and the equilibrium constants were determined. Hydrolysis is suppressed at high chloride concentrations. These results have important implications on the mode of action of the RAPTA drug candidates.
Keywords:Anticancer research   Hydrolysis   RAPTA-C   Ruthenium complex   UV-vis spectrophotometry   NMR spectroscopy
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