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A Maltol-Containing Ruthenium Polypyridyl Complex as a Potential Anticancer Agent.

  • Notaro, Anna1
  • Jakubaszek, Marta1, 2
  • Koch, Severin3
  • Rubbiani, Riccardo3
  • Dömötör, Orsolya4
  • Enyedy, Éva A4, 5
  • Dotou, Mazzarine1
  • Bedioui, Fethi6
  • Tharaud, Mickaël7
  • Goud, Bruno2
  • Ferrari, Stefano8, 9
  • Alessio, Enzo10
  • Gasser, Gilles1
  • 1 Chimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences, Laboratory for Inorganic Chemical Biology, 75005, Paris, France. , (France)
  • 2 Institut Curie, PSL University, CNRS UMR 144, 75248, Paris, France. , (France)
  • 3 Department of Chemistry, University of Zurich, Winterthurerstrasse 190, 8057, Zurich, Switzerland. , (Switzerland)
  • 4 Department of Inorganic and Analytical Chemistry, Interdisciplinary Excellence Centre, University of Szeged, Dóm tér 7., 6720, Szeged, Hungary. , (Hungary)
  • 5 MTA-SZTE Lendület Functional Metal Complexes Research Group, University of Szeged, Dóm tér 7, 6720, Szeged, Hungary. , (Hungary)
  • 6 Chimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences, Team Synthèse Electrochimie, Imagerie et Systèmes, Analytiques pour le Diagnostic, 75005, Paris, France. , (France)
  • 7 Université de Paris, Institut de physique du globe de Paris, CNRS, 75005, Paris, France. , (France)
  • 8 Institute of Molecular Cancer Research, University of Zurich, 8057, Zurich, Switzerland. , (Switzerland)
  • 9 Institute of Molecular Genetics, Czech Academy of Sciences, Videnska 1083, 14300, Prague, Czech Republic. , (Czechia)
  • 10 Department of Chemical and Pharmaceutical Sciences, University of Trieste, Via, L. Giorgieri 1, 34127, Trieste, Italy. , (Italy)
Published Article
Chemistry - A European Journal
Wiley (John Wiley & Sons)
Publication Date
Feb 17, 2020
DOI: 10.1002/chem.201904877
PMID: 32065454


Cancer is one of the main causes of death worldwide. Chemotherapy, despite its severe side effects, is to date one of the leading strategies against cancer. Metal-based drugs present several potential advantages when compared to organic compounds and they have gained trust from the scientific community after the approval on the market of the drug cisplatin. Recently, we reported the ruthenium complex ([Ru(DIP)2 (sq)](PF6 ) (where DIP is 4,7-diphenyl-1,10-phenantroline and sq is semiquinonate) with a remarkable potential as chemotherapeutic agent against cancer, both in vitro and in vivo. In this work, we analyse a structurally similar compound, namely [Ru(DIP)2 (mal)](PF6 ), carrying the flavour-enhancing agent approved by the FDA, maltol (mal). To possess an FDA approved ligand is crucial for a complex, whose mechanism of action might include ligand exchange. Herein, we describe the synthesis and characterisation of [Ru(DIP)2 (mal)](PF6 ), its stability in solutions and under conditions that resemble the physiological ones, and its in-depth biological investigation. Cytotoxicity tests on different cell lines in 2D model and on HeLa MultiCellular Tumour Spheroids (MCTS) demonstrated that our compound has higher activity than cisplatin, inspiring further tests. [Ru(DIP)2 (mal)](PF6 ) was efficiently internalised by HeLa cells through a passive transport mechanism and severely affected the mitochondrial metabolism. © 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

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