RT info:eu-repo/semantics/article
T1 Development of Cu(II) complexes of substituted polypyridyl and salicylaldehyde ligands as anticancer agents
A1 Amiri Rudbari, Hadi
A1 Kazemi, Zahra
A1 Nicosia, Angelo
A1 Mineo, Placido
A1 Riera, Chiara
A1 Rossi, Arianna
A1 Montesi, Monica
A1 Panseri, Silvia
A1 Di Pietro, Maria Letizia
A1 Iraci, Nunzio
A1 Stagno, Claudio
A1 Sorace, Lorenzo
A1 Cuevas Vicario, José Vicente
A1 Micale, Nicola
K1 Copper complexes
K1 Cancer
K1 ROS
K1 DNA-intercalation
K1 G-quadruplex stabilization
K1 Compuestos complejos
K1 Complex compounds
K1 Cáncer
K1 Cancer
AB A comprehensive panel of mixed ligand Cu(II)-complexes with general formula Cu(X-dppz)(X2-sal)(NO3) was synthesized and properly characterized through elemental analysis, FT-IR, mass spectrometry, UV–Vis and EPR spectroscopy. Theoretical calculations using DFT and TD-DFT methods were carried out to support the interpretation of the absorption spectra, revealing that most of the observed absorptions exhibit either Ligand Centered (LC) or Ligand-to-Ligand Charge Transfer (LLCT) character. The study was aimed to investigate them as anticancer agents against three cancer cell lines selected based on the incidence (MDA-MB 231) and aggressiveness (U87 and MG 63) of the related tumor type, and to investigate the effect of substitutions on both ligands (i.e., the polypyridyl diimine ligand, dppz, and the auxiliary ligand, sal) on antiproliferative activities of the complexes. The results showed that complexes bearing the –NO₂ group on the dppz ligand exhibited significantly higher cytotoxicity, particularly against MDA-MB 231 cells, compared to their Cl-substituted counterparts, with the exception of the complex with the 3-bromo-5-chloro-salicylaldehyde as auxiliary ligand. The latter also turned out to be essential for the cytotoxicity (comparative analysis with sal-free Cu(II)-complexes) as well as the complete structure of the complexes (comparative analysis with pure polypyridyl ligands). Mechanistic studies (in vitro and in silico) revealed that these complexes induce cytotoxicity through Reactive Oxygen Species (ROS) generation and intercalation into the DNA double helix, as well as through G-quadruplex stabilization. Among the synthesized compounds, complexes Cl2CuBrCl (4) and NO2CuBrCl (14) demonstrated the most promising biological activity, making them compelling candidates for further investigation as anticancer agents.
PB Elsevier
SN 1387-7003
YR 2026
FD 2026-12
LK https://hdl.handle.net/10259/12304
UL https://hdl.handle.net/10259/12304
LA eng
DS Repositorio Institucional de la Universidad de Burgos
RD 28-oct-2026