Control over where and how chemotherapeutic agents react in a patient is a key component to developing new drugs that limit side effects and maintain high efficacy. This control can be achieved by using light to activate an inert drug to generate cytotoxic species. This method of activation can be achieved through either photodynamic therapy (PDT) or photoactivated chemotherapy (PACT). PDT uses inactive photosensitizers to generate singlet oxygen and other reactive oxygen species upon light irradiation. PACT, in contrast converts an inert prodrug to a toxic new chemical entity through the cleavage of select bonds when irradiated with light. Photosensitizers that are currently used in the clinic, suffer from poor performance due to low aqueous solubility as well as side effects resulting from slow drug clearance from the body. Ruthenium(II) complexes have been demonstrated to be promising new photosensitizers and anticancer agents due to their increased solubility and tunable photophysics. A series of Ru(II) complexes containing bidentate and tridentate N-heterocyclic carbenes will be described, along with complexes containing strained ligands. These complexes show promising anticancer properties, with low toxicity, (IC50 &gt; 100 µM) in the absence of light, and good activity (IC50 values &lt; 7 µM) in the presence of light. This study will report the synthesis, photophysics, cellular localization, and anticancer properties for a series of photoactive Ru(II) complexes.

Anticancer properties of ruthenium(II) complexes and their application for photodynamic therapy and photoactivated chemotherapy

256th National Meeting (2018)

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