The current study investigates [Ru(bipy) 2 (dpphen)]-Cl 2 [where bipy = 2,2′-bipyridine and dpphen = 2,9-diphenyl-1,10-phenanthroline] (complex 1) for photoactivatable chemotherapy (PACT) application on five cancer cell lines.[Ru(bipy) 2 (phen)]Cl 2 [where phen = 1,10-phenanthroline] (complex 2) was included as an unstrained control. Upon excitation with visible light, complex 2 proved to be photostable while complex 1 underwent a quantitative dissociation of the bipy ligand and formation of a Ru II polypyridyl aqua complex in water. Complex 1 demonstrated only marginal activity in the dark; its cytotoxicity increased significantly upon photoactivation with a high phototoxicity index (PI = [IC 50 dark]/[IC 50 light]) [a]

A strained Ru(ii) prodrug exhibited enhanced cellular uptake and phototoxicity due to its lipophilic properties.

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