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Fine-Tuning the Activation Mode of an 1,3-Indandione-Based Ruthenium(II)-Cymene Half-Sandwich Complex by Variation of Its Leaving Group

1
Institute of Inorganic Chemistry, Faculty of Chemistry, University of Vienna, Waehringer Straße 42, A-1090 Vienna, Austria
2
Research Cluster “Translational Cancer Therapy Research”, University of Vienna, Waehringer Straße 42, A-1090 Vienna, Austria
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(13), 2373; https://doi.org/10.3390/molecules24132373
Received: 30 May 2019 / Revised: 21 June 2019 / Accepted: 22 June 2019 / Published: 27 June 2019
(This article belongs to the Special Issue Medicinal Importance of Ruthenium Compounds)
Fine-tuning of the properties of a recently reported 1,3-indandione-based organoruthenium complex is attempted to optimize the stability under physiological conditions. Previous work has shown its capacity of inhibiting topoisomerase IIα; however, fast aquation leads to undesired reactions and ligand cleavage in the blood stream before the tumor tissue is reached. Exchange of the chlorido ligand for six different N-donor ligands resulted in new analogs that were stable at pH 7.4 and 8.5. Only a lowered pH level, as encountered in the extracellular space of the tumor tissue, was capable of aquating the complexes. The 50% inhibitory concentration (IC50) values in three human cancer cell lines differed only slightly, and their dependence on the utilized leaving group was smaller than what would be expected from their differences in cellular accumulation, but in accordance with the very minor variation revealed in measurements of the complexes’ lipophilicity. View Full-Text
Keywords: half-sandwich complexes; ruthenium(II)–arene complexes; leaving group variation; anticancer drugs half-sandwich complexes; ruthenium(II)–arene complexes; leaving group variation; anticancer drugs
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Mokesch, S.; Schwarz, D.; Hejl, M.; Klose, M.H.M.; Roller, A.; Jakupec, M.A.; Kandioller, W.; Keppler, B.K. Fine-Tuning the Activation Mode of an 1,3-Indandione-Based Ruthenium(II)-Cymene Half-Sandwich Complex by Variation of Its Leaving Group. Molecules 2019, 24, 2373.

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