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

preprint
submitted on 21.10.2019 and posted on 25.10.2019 by Anna Notaro, Marta Jakubaszek, Severin Koch, Riccardo Rubbiani, Orsolya Dömötör, Eva Enyedy, Mazzarine Dotou, Fethi Bedioui, Mickaël Tharaud, Bruno Goud, Stefano Ferrari, Enzo Alessio, Gilles Gasser
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 ones and gained trust from the scientific community after the approval on the market of the drug cisplatin. Recently, we reported a ruthenium complex ([Ru(DIP)2(sq)](PF6), where DIP is 4,7- diphenyl-1,10-phenantroline and sq is the 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 in conditions which 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 compared to the approved drug 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.

History

Email Address of Submitting Author

gilles.gasser@chimieparistech.psl.eu

Institution

Chimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences

Country

France

ORCID For Submitting Author

0000-0002-4244-5097

Declaration of Conflict of Interest

N/A.

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in Chemistry - A European Journal

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