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- Title
Photocytotoxic Copper(II) Complexes with Schiff‐Base Scaffolds for Photodynamic Therapy.
- Authors
Lin, Rong‐Kai; Chiu, Chin‐I; Hsu, Cho‐Han; Lai, Ying‐Ju; Venkatesan, Parthiban; Huang, Po‐Han; Lai, Ping‐Shan; Lin, Chu‐Chieh
- Abstract
Abstract: 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(R<bold>QYMP</bold>)(dppn)] (R<bold>QYMP</bold>=<italic>N</italic>,<italic>N</italic>,<italic>O</italic>‐tridentate Schiff‐base derivatives, dppn=benzo[<italic>i</italic>]dipyrido[3,2‐<italic>a</italic>;2′,3′‐<italic>c</italic>]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(cumyl<bold>QYMP</bold>)(dppn)](ClO4) complex (<bold>3</bold>) 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‐OMe<bold>QYMP</bold>)(dppn)](ClO4) (<bold>4</bold>). This can be attributed to the formation of reactive oxygen species, cell apoptosis, and caspase‐3 activation, indicating high potential of complex <bold>4</bold> 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.
- Subjects
PHOTODYNAMIC therapy; PHOTOSENSITIZERS; COPPER; IRRADIATION; FOURIER transform infrared spectroscopy
- Publication
Chemistry - A European Journal, 2018, Vol 24, Issue 16, p4111
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201705640