Photodynamic therapy (PDT) is a promising and minimally invasive method for the treatment of superficial diseases, and photosensitizers with high phototoxicity indices (defined as (IC50dark)/(IC50irradiation)) are essential for the development of ideal photosensitizing properties for this technology. Herein, we report a series of photocytotoxic copper(II) complexes [Cu(RQYMP)(dppn)] (RQYMP=N,N,O‐tridentate Schiff‐base derivatives, dppn=benzo[i]dipyrido[3,2‐a;2′,3′‐c]phenazine), the structures of which have been confirmed by mass spectrometry and FTIR spectroscopy. X‐ray crystallography revealed that the CuN4O core of the [Cu(cumylQYMP)(dppn)](ClO4) complex (3) has a distorted square‐pyramidal geometry. Phototoxicity indices of 329 against human squamous cell carcinoma (SCC15) and 296 against basal cell carcinoma (BCC) cell lines have been determined with [Cu(3‐OMeQYMP)(dppn)](ClO4) (4). This can be attributed to the formation of reactive oxygen species, cell apoptosis, and caspase‐3 activation, indicating high potential of complex 4 as a photosensitizer candidate in PDT. Thus, copper complexes bearing suitable Schiff‐base ligands with a dppn co‐ligand may be considered for the design of efficient metal‐based anticancer agents for PDT.
Chemistry - A European Journal – Wiley
Published: Jan 15, 2018
Keywords: ; ; ; ;
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