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Eur J Med Chem ; 132: 282-293, 2017 May 26.
Article in English | MEDLINE | ID: mdl-28371640

ABSTRACT

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 antiproliferative 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(η6-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 µM) 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 µM.


Subject(s)
Antineoplastic Agents/chemistry , Organometallic Compounds/chemistry , Ruthenium/chemistry , Animals , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , Cisplatin/pharmacology , Humans , Hydrophobic and Hydrophilic Interactions , Ligands , Nitrogen Oxides , Organometallic Compounds/pharmacology , Structure-Activity Relationship , Zebrafish/embryology
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