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Pharmaceuticals
Volume 13
Issue 12
10.3390/ph13120471
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Article

Conjugates Containing Two and Three Trithiolato-Bridged Dinuclear Ruthenium(II)-Arene Units as In Vitro Antiparasitic and Anticancer Agents

by
Valentin Studer
1,†,
Nicoleta Anghel
2,†,
Oksana Desiatkina
1,
Timo Felder
1,
Ghalia Boubaker
2,
Yosra Amdouni
2,3,
Jessica Ramseier
2,
Martin Hungerbühler
4,5,
Christoph Kempf
4,5,
Johannes Thomas Heverhagen
4,5,
Andrew Hemphill
2,*,
Nico Ruprecht
4,5,*,
Julien Furrer
1,* and
Emilia Păunescu
1,*
1
Department of Chemistry and Biochemistry, University of Bern, Freiestrasse 3, CH-3012 Bern, Switzerland
2
Vetsuisse Faculty, Institute of Parasitology, University of Bern, Länggassstrasse 122, CH-3012 Bern, Switzerland
3
Laboratoire de Parasitologie, Institution de la Recherche et de l’Enseignement Supérieur Agricoles, École Nationale de Médecine Vétérinaire de Sidi Thabet, University of Manouba, Sidi Thabet 2020, Tunisia
4
Department of BioMedical Research, Experimental Radiology, University of Bern, CH-3008 Bern, Switzerland
5
Department of Diagnostic, Interventional and Pediatric Radiology, Bern University Hospital, University of Bern, CH-3010 Bern, Switzerland
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Pharmaceuticals 2020, 13(12), 471; https://doi.org/10.3390/ph13120471
Received: 11 November 2020 / Revised: 10 December 2020 / Accepted: 11 December 2020 / Published: 16 December 2020
(This article belongs to the Special Issue Metal-Based Drugs: Updates and Perspectives)
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Abstract

The synthesis, characterization, and in vitro antiparasitic and anticancer activity evaluation of new conjugates containing two and three dinuclear trithiolato-bridged ruthenium(II)-arene units are presented. Antiparasitic activity was evaluated using transgenic Toxoplasmagondii tachyzoites constitutively expressing β-galactosidase grown in human foreskin fibroblasts (HFF). The compounds inhibited T.gondii proliferation with IC50 values ranging from 90 to 539 nM, and seven derivatives displayed IC50 values lower than the reference compound pyrimethamine, which is currently used for treatment of toxoplasmosis. Overall, compound flexibility and size impacted on the anti-Toxoplasma activity. The anticancer activity of 14 compounds was assessed against cancer cell lines A2780, A2780cisR (human ovarian cisplatin sensitive and resistant), A24, (D-)A24cisPt8.0 (human lung adenocarcinoma cells wild type and cisPt resistant subline). The compounds displayed IC50 values ranging from 23 to 650 nM. In A2780cisR, A24 and (D-)A24cisPt8.0 cells, all compounds were considerably more cytotoxic than cisplatin, with IC50 values lower by two orders of magnitude. Irrespective of the nature of the connectors (alkyl/aryl) or the numbers of the di-ruthenium units (two/three), ester conjugates 6–10 and 20 exhibited similar antiproliferative profiles, and were more cytotoxic than amide analogues 11–14, 23, and 24. Polynuclear conjugates with multiple trithiolato-bridged di-ruthenium(II)-arene moieties deserve further investigation. View Full-Text
Keywords: bioactive organometallics; polynuclear ruthenium compounds; antiparasitic; anticancer bioactive organometallics; polynuclear ruthenium compounds; antiparasitic; anticancer
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MDPI and ACS Style

Studer, V.; Anghel, N.; Desiatkina, O.; Felder, T.; Boubaker, G.; Amdouni, Y.; Ramseier, J.; Hungerbühler, M.; Kempf, C.; Heverhagen, J.T.; Hemphill, A.; Ruprecht, N.; Furrer, J.; Păunescu, E. Conjugates Containing Two and Three Trithiolato-Bridged Dinuclear Ruthenium(II)-Arene Units as In Vitro Antiparasitic and Anticancer Agents. Pharmaceuticals 2020, 13, 471. https://doi.org/10.3390/ph13120471

AMA Style

Studer V, Anghel N, Desiatkina O, Felder T, Boubaker G, Amdouni Y, Ramseier J, Hungerbühler M, Kempf C, Heverhagen JT, Hemphill A, Ruprecht N, Furrer J, Păunescu E. Conjugates Containing Two and Three Trithiolato-Bridged Dinuclear Ruthenium(II)-Arene Units as In Vitro Antiparasitic and Anticancer Agents. Pharmaceuticals. 2020; 13(12):471. https://doi.org/10.3390/ph13120471

Chicago/Turabian Style

Studer, Valentin, Nicoleta Anghel, Oksana Desiatkina, Timo Felder, Ghalia Boubaker, Yosra Amdouni, Jessica Ramseier, Martin Hungerbühler, Christoph Kempf, Johannes Thomas Heverhagen, Andrew Hemphill, Nico Ruprecht, Julien Furrer, and Emilia Păunescu. 2020. "Conjugates Containing Two and Three Trithiolato-Bridged Dinuclear Ruthenium(II)-Arene Units as In Vitro Antiparasitic and Anticancer Agents" Pharmaceuticals 13, no. 12: 471. https://doi.org/10.3390/ph13120471

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