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A Dual Killing Strategy - Photocatalytic Generation of Singlet Oxygen with Concomitant Pt(IV) Prodrug Activation.

A Ruthenium-based mitochondrial-targeting photosensitiser that undergoes efficient cell uptake, enables the rapid catalytic conversion of Pt(IV) prodrugs into their active Pt(II) counterparts and drives the generation of singlet oxygen was designed. This duality drives two orthogonal killing mechanisms with cytotoxicity mediated with temporal and spatial control and was shown to elicit cell death of a panel of cancer cell lines including those showing oxaliplatin-resistance.