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• W2076497239 abstract "RuII(arene) complexes have been shown to be promising anticancer agents, capable of overcoming major drawbacks of currently used chemotherapeutics. We have synthesized RuII(η6-arene) compounds carrying bioactive flavonol ligands with the aim to obtain multitargeted anticancer agents. To validate this concept, studies on the mode of action of the complexes were conducted which indicated that they form covalent bonds to DNA, have only minor impact on the cell cycle, but inhibit CDK2 and topoisomerase IIα in vitro. The cytotoxic activity was determined in human cancer cell lines, resulting in very low IC50 values as compared to other RuII(arene) complexes and showing a structure-activity relationship dependent on the substitution pattern of the flavonol ligand. Furthermore, the inhibition of cell growth correlates well with the topoisomerase inhibitory activity. Compared to the flavonol ligands, the RuII(η6-p-cymene) complexes are more potent antiproliferative agents, which can be explained by potential multitargeted properties." @default.
• W2076497239 created "2016-06-24" @default.
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• W2076497239 date "2012-11-19" @default.
• W2076497239 modified "2023-10-03" @default.
• W2076497239 title "Structure–Activity Relationships of Targeted Ru^II(η⁶-<i>p</i>-Cymene) Anticancer Complexes with Flavonol-Derived Ligands" @default.
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• W2076497239 doi "https://doi.org/10.1021/jm301376a" @default.
• W2076497239 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23134291" @default.
• W2076497239 hasPublicationYear "2012" @default.
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