Title:
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Copper(II) N, N, O -Chelating Complexes as Potential Anticancer Agents
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Author:
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Peña, Quim; Sciortino, Giuseppe; Maréchal, Jean-Didier; Bertaina, Sylvain; Simaan, A. Jalila; Lorenzo Rivera, Julia; Capdevila Vidal, Mercè; Bayón Rueda, Joan Pau; Iranzo, Olga; Palacios Bonilla, Òscar; Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular
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Abstract:
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Altres ajuts: acords transformatius de la UAB |
Abstract:
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Three novel dinuclear Cu(II) complexes based on a N,N,O-chelating salphen-like ligand scaffold and bearing varying aromatic substituents (−H, −Cl, and −Br) have been synthesized and characterized. The experimental and computational data obtained suggest that all three complexes exist in the dimeric form in the solid state and adopt the same conformation. The mass spectrometry and electron paramagnetic resonance results indicate that the dimeric structure coexists with the monomeric form in solution upon solvent (dimethyl sulfoxide and water) coordination. The three synthesized Cu(II) complexes exhibit high potentiality as ROS generators, with the Cu(II)/Cu(I) redox potential inside the biological redox window, and thus being able to biologically undergo Cu(II)/Cu(I) redox cycling. The formation of ROS is one of the most promising reported cell death mechanisms for metal complexes to offer an inherent selectivity to cancer cells. In vitro cytotoxic studies in two different cancer cell lines (HeLa and MCF7) and in a normal fibroblast cell line show promising selective cytotoxicity for cancer cells (IC50 about 25 μM in HeLa cells, which is in the range of cisplatin and improved with respect to carboplatin), hence placing this N,N,O-chelating salphen-like metallic core as a promising scaffold to be explored in the design of future tailor-made Cu(II) cytotoxic compounds. |
Rights:
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open access
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https://creativecommons.org/licenses/by/4.0/ |
Document type:
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Article |
Published by:
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Uri:
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https://ddd.uab.cat/record/249952
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