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Herein, we construct a series of Ru(II) metallacycles with multimodal chemo-phototherapeutic properties, which exhibited much higher anticancer activity and better cancer-cell selectivity than cisplatin. The antitumor mechanism could be ascribed to the activation of caspase 3/7 and the resulting apoptosis. These results open new possibilities for Ru(II) metallacycles in biomedicine.

Graphical abstract: Rationally designed Ru(ii) metallacycles with tunable imidazole ligands for synergistical chemo-phototherapy of cancer

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