Many Ru(II) complexes can undergo photoinduced ligand dissociation in aqueous solutions, and the formed aqua Ru(II) species may bind to DNA covalently. This property has been applied to develop novel photoactivated chemotherapy (PACT) agents for cancer treatment in recent years. By finely tuning ligand structures and coordination configurations, PACT may realize highly selective and on-demand release of active species in cancer tissues, leading to an improved efficacy and diminished side effects. In this review, the progress in Ru(II)-based PACT agents was fully discussed and a perspective for their future development was included.
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