Journal
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
Volume -, Issue 12, Pages 1687-1694Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejic.201601450
Keywords
Synthesis; Photochemistry; Cytotoxicity; DNA damage; Ruthenium
Categories
Funding
- National Institutes of Health [5R01GM107586]
- National Science Foundation (NSF) [MRI CHE-0319176]
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Ruthenium complexes capable of light-triggered cytotoxicity are appealing potential prodrugs for photodynamic therapy (PDT) and photoactivated chemotherapy (PACT). Two groups of (polypyridyl) Ru-II complexes with 2-(2-pyridyl) benzazole ligands were synthesized and investigated for their photochemical properties and anticancer activity to compare strained and unstrained systems that are likely to have different biological mechanisms of action. The structure-activity relationship was focused on the benzazole-core bioisosterism and replacement of coligands in RuII complexes. Strained compounds rap-idly ejected the 2-(2-pyridyl) benzazole ligand after light irradiation, and possessed strong toxicity in the HL-60 cell line both under dark and light conditions. In contrast, unstrained RuII complexes were nontoxic in the absence of light, induced cytotoxicity at nanomolar concentrations after light irradiation, and were capable of light-induced DNA damage. The 90-220-fold difference in light and dark IC50 values provides a large potential therapeutic window to allow for selective targeting of cells by exposure to light.
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