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Ruthenium(II) Complex Containing a Redox-Active Semiquinonate Ligand as a Potential Chemotherapeutic Agent : From Synthesis to In Vivo Studies

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2020

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Notaro, Anna
Frei, Angelo
Rubbiani, Riccardo
Jakubaszek, Marta
Basu, Uttara
Koch, Severin
Mari, Cristina
Gasser, Gilles
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https://doi.org/10.1021/acs.jmedchem.0c00431
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Journal of Medicinal Chemistry. American Chemical Society (ACS). 2020, 63(10), pp. 5568-5584. ISSN 0095-9065. eISSN 1943-2992. Available under: doi: 10.1021/acs.jmedchem.0c00431

Zusammenfassung

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) (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.

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540 Chemie

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ISO 690NOTARO, Anna, Angelo FREI, Riccardo RUBBIANI, Marta JAKUBASZEK, Uttara BASU, Severin KOCH, Cristina MARI, Nils ROTTHOWE, Rainer F. WINTER, Gilles GASSER, 2020. Ruthenium(II) Complex Containing a Redox-Active Semiquinonate Ligand as a Potential Chemotherapeutic Agent : From Synthesis to In Vivo Studies. In: Journal of Medicinal Chemistry. American Chemical Society (ACS). 2020, 63(10), pp. 5568-5584. ISSN 0095-9065. eISSN 1943-2992. Available under: doi: 10.1021/acs.jmedchem.0c00431
BibTex
@article{Notaro2020Ruthe-52321,
  year={2020},
  doi={10.1021/acs.jmedchem.0c00431},
  title={Ruthenium(II) Complex Containing a Redox-Active Semiquinonate Ligand as a Potential Chemotherapeutic Agent : From Synthesis to In Vivo Studies},
  number={10},
  volume={63},
  issn={0095-9065},
  journal={Journal of Medicinal Chemistry},
  pages={5568--5584},
  author={Notaro, Anna and Frei, Angelo and Rubbiani, Riccardo and Jakubaszek, Marta and Basu, Uttara and Koch, Severin and Mari, Cristina and Rotthowe, Nils and Winter, Rainer F. and Gasser, Gilles}
}
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