Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 132, Issue -, Pages 282-293Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.03.029
Keywords
Ruthenium.complexes; Antiproliferative activity; Lipophilicity; Cancer; In vivo toxicity; Zebrafish
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Funding
- INRS University
- Fonds de Recherche en Sante du Quebec (Etablissement de Jeunes Chercheurs) [32622]
- Canada Foundation for Innovation [34846]
- Armand-Frappier Foundation of INRS University
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Ru(II)-arene complexes are attracting increasing attention due to their considerable antitumoral activity. However, it is difficult to clearly establish a direct relationship between their structure and anti proliferative activity, as substantial structural changes might not only affect their anticancer activity but also tightly control their activation site(s) and/or their biological target(s). Herein, we describe the synthesis and characterization of four ruthenium(II) arene complexes bearing bidentate N,O-donor Schiff-base ligands ([Ru(eta(6)-benzene)(N-O)Cl]) that display a significantly distinct antiproliferative activity against cancer cells, despite their close structural similarity. Furthermore, we suggest there is a link between their respective antiproliferative activity and their lipophilicity, as the latter affects their ability to accumulate into cancer cells. This lipophilicity-cytotoxicity relationship was exploited to design another structurally related ruthenium complex with a much higher antiproliferative activity (IC50 > 25.0 mu M) against three different human cancer cell lines. Whereas this complex shows a slightly lower activity than that of clinically approved cis-platin against the same human cancer cell lines, it displays a lower toxicity in zebrafish (Danio rerio) embryos at concentrations up to 20 mu M. (C) 2017 Elsevier Masson SAS. All rights reserved.
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