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New Luminescent Polynuclear Metal Complexes with Anticancer Properties: Toward Structure–Activity Relationships

Abstract : A series of new heterodinuclear luminescent complexes with two different organic ligands have been synthesized and characterized. A luminescent Ru-II(polypyridine) moiety and a metal-based anticancer fragment (AuCl, (p-cymene)RuCl2, (p-cymene)OsCl2, (Cp*)RhCl2, or Au-thioglucose) are the two general features of these complexes. All of the bimetallic compounds have been evaluated for their antiproliferative properties in vitro in human cancer cell lines. Only the complexes containing an Au(I) fragment exhibit antiproliferative activity in the range of cisplatin or higher. The photophysical and electrochemical properties of the bimetallic species have been investigated, and fluorescence microscopy experiments have been performed successfully. The most promising bimetallic cytotoxic complexes (i.e., with the Au-thioglucose scaffold) have shown to be easily taken up by cancer cells at 37 degrees C in the cytoplasm or in specific organelles. Interestingly, experiments repeated at 4 degrees C showed no uptake of the bimetallic species inside cells, which confirms involvement of active transport processes. To evaluate the role of glucose transporters in the cell uptake of the gold complexes, inhibition of the GluT-1 (glucose transporter isoform with high level of expression in cancer cells) was achieved, showing only scarce influence on the compounds' uptake. Finally, the observed absence of interactions with nucleic acid model structures suggests that the gold compounds may have different intracellular targets with respect to cisplatin.
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Contributeur : ICMUB - université de Bourgogne Connectez-vous pour contacter le contributeur
Soumis le : vendredi 25 novembre 2016 - 10:32:42
Dernière modification le : vendredi 14 octobre 2022 - 04:05:36

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Margot Wenzel, Andreia de Almeida, Emilia Bigaeva, Paul Kavanagh, Michel Picquet, et al.. New Luminescent Polynuclear Metal Complexes with Anticancer Properties: Toward Structure–Activity Relationships. Inorganic Chemistry, 2016, 55 (5), pp.2544 - 2557. ⟨10.1021/acs.inorgchem.5b02910⟩. ⟨hal-01402767⟩



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