Dinuclear copper(II) complexes with a bridging bis(chalcone) ligand reveal considerable in vitro cytotoxicity on human cancer cells and enhanced selectivity

Trávníček, Zdeněk; Vančo, Ján; Belza, Jan; Zoppellaro, Giorgio; Dvořák, Zdeněk

doi:10.1016/j.jinorgbio.2024.112481

Journal of Inorganic Biochemistry

2024

DOI: 10.1016/j.jinorgbio.2024.112481

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Dinuclear copper(II) complexes with a bridging bis(chalcone) ligand reveal considerable in vitro cytotoxicity on human cancer cells and enhanced selectivity

Zdeněk Trávníček,

Ján Vančo,

Jan Belza

et al.

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Cited by 3 publications

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Synthesis of N-alkyl azoles carrying metal complexes for catalytic and medicinal applications

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Phenanthroline and phenyl carboxylate mixed ligand copper complexes in developing drugs to treat cancer

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The Induction of G2/M Phase Cell Cycle Arrest and Apoptosis by the Chalcone Derivative 1C in Sensitive and Resistant Ovarian Cancer Cells Is Associated with ROS Generation

Salanci,

Vilková,

Martinez

et al. 2024

IJMS

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Ovarian cancer ranks among the most severe forms of cancer affecting the female reproductive organs, posing a significant clinical challenge primarily due to the development of resistance to conventional therapies. This study investigated the effects of the chalcone derivative 1C on sensitive (A2780) and cisplatin-resistant (A2780cis) ovarian cancer cell lines. Our findings revealed that 1C suppressed cell viability, induced cell cycle arrest at the G2/M phase, and triggered apoptosis in both cell lines. These effects are closely associated with generating reactive oxygen species (ROS). Mechanistically, 1C induced DNA damage, modulated the activity of p21, PCNA, and phosphorylation of Rb and Bad proteins, as well as cleaved PARP. Moreover, it modulated Akt, Erk1/2, and NF-κB signaling pathways. Interestingly, we observed differential effects of 1C on Nrf2 levels between sensitive and resistant cells. While 1C increased Nrf2 levels in sensitive cells after 12 h and decreased them after 48 h, the opposite effect was observed in resistant cells. Notably, most of these effects were suppressed by the potent antioxidant N-acetylcysteine (NAC), underscoring the crucial role of ROS in 1C-induced antiproliferative activity. Moreover, we suggest that modulation of Nrf2 levels can, at least partially, contribute to the antiproliferative effect of chalcone 1C.

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Dinuclear copper(II) complexes with a bridging bis(chalcone) ligand reveal considerable in vitro cytotoxicity on human cancer cells and enhanced selectivity

Cited by 3 publications

References 45 publications

Synthesis of N-alkyl azoles carrying metal complexes for catalytic and medicinal applications

Synthesis of N-alkyl azoles carrying metal complexes for catalytic and medicinal applications

Phenanthroline and phenyl carboxylate mixed ligand copper complexes in developing drugs to treat cancer

The Induction of G2/M Phase Cell Cycle Arrest and Apoptosis by the Chalcone Derivative 1C in Sensitive and Resistant Ovarian Cancer Cells Is Associated with ROS Generation

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