Next Article in Journal
Zinc(II) as a Versatile Template for Efficient Dipolar and Octupolar Second-Order Nonlinear Optical Molecular Materials §
Next Article in Special Issue
Investigation of 1-Methylcytosine as a Ligand in Gold(III) Complexes: Synthesis and Protein Interactions
Previous Article in Journal
State of the Art of Boron and Tin Complexes in Second- and Third-Order Nonlinear Optics §
Previous Article in Special Issue
Development and Validation of Liquid Chromatography-Based Methods to Assess the Lipophilicity of Cytotoxic Platinum(IV) Complexes
Open AccessArticle

Anti-Proliferative and Anti-Migration Activity of Arene–Ruthenium(II) Complexes with Azole Therapeutic Agents

1
Departamento de Química, Universidade Federal de São Carlos, CEP 13565-905 São Carlos, SP, Brazil
2
Instituto Federal Goiano—IFG, Campus Ceres, CEP 76300-00 Ceres, GO, Brazil
3
Departamento de Gerontologia, Universidade Federal de São Carlos, CEP 13565-905 São Carlos, SP, Brazil
4
Instituto Nacional de Metrologia, Qualidade e Tecnologia, INMETRO, CEP 25250-020 Xerem, RJ, Brazil
5
Departamento de Química, ICE, Universidade Federal de Juiz de Fora, CEP 36036-900 Juiz de Fora, MG, Brazil
*
Authors to whom correspondence should be addressed.
Inorganics 2018, 6(4), 132; https://doi.org/10.3390/inorganics6040132
Received: 24 October 2018 / Revised: 3 December 2018 / Accepted: 5 December 2018 / Published: 11 December 2018
The efficacy of organoruthenium complexes containing ergosterol biosynthesis inhibitors (CTZ: clotrimazole, KTZ: ketoconazole and FCZ: fluconazole) against tumor cells, and their interaction with important macro-biomolecules such as human serum albumin and DNA have been investigated here. Our experimental results indicated that these ruthenium(II) complexes present spontaneous electrostatic interactions with albumin, and act as minor groove binders with the DNA. The ability of these Ru(II)–azole complexes to inhibit the proliferation of selected human tumor and non-tumor cell lines was determined by MTT assay. Complexes [RuCl(CTZ)(η6-p-cymene)(PPh3)]PF6 (3) and [RuCl(KTZ)(η6-p-cymene)(PPh3)]PF6 (4) were shown to be between 3- and 40-fold more cytotoxic than the free ligands and the positive control cisplatin. Complex 3 was selected to continue studies on the triple negative breast tumor cell line MDA-MB-231, inducing morphological changes, loss of adhesion, inhibition of colony formation, and migration through Boyden chambers, cell cycle arrest in the sub-G1 phase, and a mechanism of cell death by apoptosis. All these interesting results show the potential of this class of organometallic Ru(II) complexes as an antiproliferative agent. View Full-Text
Keywords: ruthenium complexes; antiproliferative; antimigration; DNA interaction; HSA binding ruthenium complexes; antiproliferative; antimigration; DNA interaction; HSA binding
Show Figures

Graphical abstract

MDPI and ACS Style

Colina-Vegas, L.; Oliveira, K.M.; Cunha, B.N.; Cominetti, M.R.; Navarro, M.; Azevedo Batista, A. Anti-Proliferative and Anti-Migration Activity of Arene–Ruthenium(II) Complexes with Azole Therapeutic Agents. Inorganics 2018, 6, 132.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop