Phototherapy is a medical treatment that uses light to “turn on” drug molecules, potentially reducing off-target damage by spatially restricting the areas exposed to radiation. Traditionally, photoactive molecules sensitize oxygen to produce singlet oxygen as the cytotoxic species, limiting their use in hypoxic tumors. Ru(II) polypyridyl complexes have tunable photophysical and photochemical traits that can be exploited to design complexes that are inert until irradiated with visible light. Incorporation of photochemically labile ligands results in light activated ligand dissociation, producing an active species that is capable of reacting with biomolecules resulting in a cytotoxic response. Many factors can influence the efficacy of photoactive drug molecules and we aimed to identify important structural features for Ru(II) complexes used in phototherapy. The photochemical reactivity, DNA interaction, and cytotoxicity was studied for a series of mono- and di-functional Ru(II) complexes. Additionally, the influence of geometry was tested for a series of di-functional Ru(II) complexes. The results show distinct differences based on each structural feature and provides information that can be used to rationally design new Ru(II) polypyridyl complexes for their application in phototherapy.

Structural features that influence photochemical reactivity and phototherapeutic activity of Ru(II) polypyridyl complexes

251st National Meeting (2016)

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