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A Maltol-Containing Ruthenium Polypyridyl Complex as a Potential Anticancer Agent
Preprints are manuscripts made publicly available before they have been submitted for formal peer review and publication. They might contain new research findings or data. Preprints can be a draft or final version of an author's research but must not have been accepted for publication at the time of submission.
submitted on 21.10.2019 and posted on 25.10.2019by 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