Triazole‐Derived Ruthenium(II) Complexes as Novel Candidates for Cancer Therapy

The first examples of Ru(II) η<sup>6</sup>-arene (benzene and p-cymene) complexes containing a bidentate triazolylidene-triazolide ligand have been prepared and fully characterized. Their antiproliferative effect has been investigated against tumour cells A2780 (ovarian carcinoma), HCT116 (colorectal carcinoma), and HCT116dox (colorectal carcinoma resistant to doxorubicin), and in human dermal fibroblasts. The Ru complex bearing the p-cymene arene group exhibited a stronger antiproliferative effect across all tested cell lines, while the benzene-containing complex displayed higher selectivity toward tumor cells. Both complexes induced apoptosis, likely through ROS production (in the benzene complex), and inhibited tumorigenic processes, including cell migration and angiogenesis. In zebrafish models, they showed strong selectivity for cancer cells with minimal toxicity to healthy cells, effectively reducing the proliferation of HCT116 colorectal cancer cells. This study provides the first in vivo evidence of the anticancer potential of Ru triazolylidenes in zebrafish models.

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Publication Details

Journal
ChemPlusChem
Published
2025-02-15
DOI
https://doi.org/10.1002/cplu.202400775
Citations
2
Primary Topic
Click Chemistry and Applications
Type
article
Field-Weighted Citation Impact
1.87

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article

Triazole‐Derived Ruthenium(II) Complexes as Novel Candidates for Cancer Therapy

Sabela F. Vila, Pedro Viana Baptista, Beatriz Royo, Laura Sánchez et al.
2 citations
ChemPlusChem
Click Chemistry and Applications
1.87
article

Triazole‐Derived Ruthenium(II) Complexes as Novel Candidates for Cancer Therapy

Sabela F. Vila, Pedro Viana Baptista, Beatriz Royo, Laura Sánchez, Álvaro J. Arana, Alexandra Ramos Fernandes, Valéria Sousa de Andrade, Jhonathan A. A. Fernández, Clara S. B. Gomes, Beatriz G. Carvalho, Sofia Friães
article en
2 citations

Abstract

The first examples of Ru(II) η<sup>6</sup>-arene (benzene and p-cymene) complexes containing a bidentate triazolylidene-triazolide ligand have been prepared and fully characterized. Their antiproliferative effect has been investigated against tumour cells A2780 (ovarian carcinoma), HCT116 (colorectal carcinoma), and HCT116dox (colorectal carcinoma resistant to doxorubicin), and in human dermal fibroblasts. The Ru complex bearing the p-cymene arene group exhibited a stronger antiproliferative effect across all tested cell lines, while the benzene-containing complex displayed higher selectivity toward tumor cells. Both complexes induced apoptosis, likely through ROS production (in the benzene complex), and inhibited tumorigenic processes, including cell migration and angiogenesis. In zebrafish models, they showed strong selectivity for cancer cells with minimal toxicity to healthy cells, effectively reducing the proliferation of HCT116 colorectal cancer cells. This study provides the first in vivo evidence of the anticancer potential of Ru triazolylidenes in zebrafish models.

ChemPlusChemVol. 90(5)
Universidade Estadual de Campinas (UNICAMP) (BR), Universidade de Santiago de Compostela (ES), Instituto de Tecnología Química (ES), Rede de Química e Tecnologia (PT), Instituto de Biologia Experimental e Tecnológica (PT), Universidade Nova de Lisboa (PT)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Ministério da Ciência, Tecnologia e Ensino Superior, Applied Molecular Biosciences Unit, Laboratório Associado para a Química Verde, Fundação para a Ciência e a Tecnologia, Instituto de Tecnologia Química e Biológica, Universidade Nova de Lisboa
Good health and well-being
Openalex Percentile: Top 18%
Click Chemistry and Applications
1.87
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