Copper(II) N, N, O -Chelating Complexes as Potential Anticancer Agents
Peña, Quim (Universitat Autònoma de Barcelona. Departament de Química)
Sciortino, Giuseppe (Universitat Autònoma de Barcelona. Departament de Química)
Maréchal, Jean-Didier (Universitat Autònoma de Barcelona. Departament de Química)
Bertaina, Sylvain (Aix-Marseille Université)
Simaan, A. Jalila (Aix-Marseille Université)
Lorenzo Rivera, Julia (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí")
Capdevila Vidal, Mercè (Universitat Autònoma de Barcelona. Departament de Química)
Bayón, Joan Carles (Universitat Autònoma de Barcelona. Departament de Química)
Iranzo, Olga (Aix-Marseille Université)
Palacios Bonilla, Òscar (Universitat Autònoma de Barcelona. Departament de Química)
Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular

Date:	2021
Abstract:	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.
Grants:	Ministerio de Economía y Competitividad BIO2015-67358- C2-2-P Ministerio de Economía y Competitividad CTQ2015-70371-REDT Agencia Estatal de Investigación RTI2018-098027-B-C22 Agència de Gestió d'Ajuts Universitaris i de Recerca 2017/SGR-864
Note:	Altres ajuts: acords transformatius de la UAB
Rights:	Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial, la distribució, la comunicació pública de l'obra i la creació d'obres derivades, fins i tot amb finalitats comercials, sempre i quan es reconegui l'autoria de l'obra original.
Language:	Anglès
Document:	Article ; recerca ; Versió publicada
Published in:	Inorganic chemistry, Vol. 60, Issue 5 (March 2021) , p. 2939-2952, ISSN 1520-510X

DOI: 10.1021/acs.inorgchem.0c02932
PMID: 33596377

14 p, 3.2 MB

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Research literature > UAB research groups literature > Research Centres and Groups (research output) > Health sciences and biosciences > Institut de Biotecnologia i de Biomedicina (IBB)
Articles > Research articles
Articles > Published articles