Copper(II) N, N, O-Chelating Complexes as Potential Anticancer Agents

Quim Peña, Giuseppe Sciortino, Jean Didier Maréchal, Sylvain Bertaina, A. Jalila Simaan, Julia Lorenzo, Mercè Capdevila, Pau Bayón, Olga Iranzo, Òscar Palacios*

*Corresponding author for this work

Research output: Contribution to journalArticleResearchpeer-review

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.

Original languageEnglish
Pages (from-to)2939-2952
Number of pages14
JournalInorganic Chemistry
Volume60
Issue number5
DOIs
Publication statusPublished - 1 Mar 2021

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