| Literature DB >> 32319768 |
Anna Notaro1, Angelo Frei2, Riccardo Rubbiani2, Marta Jakubaszek1,3, Uttara Basu1, Severin Koch2, Cristina Mari2, Mazzarine Dotou1, Olivier Blacque2, Jérémie Gouyon4, Fethi Bedioui4, Nils Rotthowe5, Rainer F Winter5, Bruno Goud3, Stefano Ferrari6,7, Mickaël Tharaud8, Martina Řezáčová9, Jana Humajová10, Pavel Tomšík9, Gilles Gasser1.
Abstract
Chemotherapy remains one of the dominant treatments to cure cancer. However, due to the many inherent drawbacks, there is a search for new chemotherapeutic drugs. Many classes of compounds have been investigated over the years to discover new targets and synergistic mechanisms of action including multicellular targets. In this work, we designed a new chemotherapeutic drug candidate against cancer, namely, [Ru(DIP)2(sq)](PF6) (Ru-sq) (DIP = 4,7-diphenyl-1,10-phenanthroline; sq = semiquinonate ligand). The aim was to combine the great potential expressed by Ru(II) polypyridyl complexes and the singular redox and biological properties associated with the catecholate moiety. Experimental evidence (e.g., X-ray crystallography, electron paramagnetic resonance, electrochemistry) demonstrates that the semiquinonate is the preferred oxidation state of the dioxo ligand in this complex. The biological activity of Ru-sq was then scrutinized in vitro and in vivo, and the results highlight the promising potential of this complex as a chemotherapeutic agent against cancer.Entities:
Mesh:
Substances:
Year: 2020 PMID: 32319768 DOI: 10.1021/acs.jmedchem.0c00431
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446