SYNTHESIS, LUMINESCENT PROPERTIES AND BIOLOGICAL ACTIVITY OF LANTANOIDE COMPLEXES WITH SUBSTITUTED 1,2,3 - TRIAZOLES
Rubrics: 1. CHEMISTRY
Authors:
1.
KNITU
Type:
Article
Pages:
from 18
to 24
Status:
Published
Received:
27.01.2026
Accepted:
28.01.2026
Published:
28.01.2026
Language:
Russian
Keywords:
1,2,3-TRIAZOLE, HETEROLIGAND COMPLEXES OF LANTHANIDES, LUMINESCENCE, SOLUBILIZATION, LYOTROPIC MESOPHASES, PLURONIC P123, CYTOTOXICITY
Abstract:
Heterocyclic compounds are of interest for the synthesis of pharmaceuticals, and the development of their delivery systems is of particular importance for improving the biopharmaceutical aspects of therapy. In this regard, substituted 1,2,3 - triazoles are of interest, as they are capable of binding to various enzymes and receptors, exhibiting high biological activity. Currently, 1,2,3-triazoles, as a class of N-heterocyclic compounds, due to their dual functionality, are used both as pharmacophores and linkers in molecular synthesis strategies. The paper presents the synthesis and properties of new chelates of europium and terbium ions with substituted 1,2,3-triazoles TR1 and TR2. Targeted synthesis of 1,2,3 - triazoles was carried out to increase solubility and improve complexation with lanthanide ions. 1,10-phenanthroline and 2,4-pentanedione were used as sensitizing chromophore ligands. The synthesized complexes exhibit high luminescent characteristics. Cellular cytotoxicity was studied for an individual ligand of 1,2,3 - triazole and terbium chelate. It is shown that bis-1,3-(4-methylcarboxyl-1,2,3-triazol-1-yl)benzene selectively acts on human duodenal adenocarcinoma cells, exhibiting high activity of 63.0 ± 4.7 μM. This compound is not toxic to human hepatocytes. The luminescent terbium complex [Tb(AcAc)3(TR2)] does not exhibit cytotoxicity in the studied cell lines and can be used as an optical probe without destructive effect on cells in vivo. Efficient solubilization of substituted 1,2,3-triazoles TR1 and TR2 and heteroligand complexes in the structure of the lyotropic mesophase Pluronic P123 / dimethylsulfoxide allows their use in biotic systems.
Heterocyclic compounds are of interest for the synthesis of pharmaceuticals, and the development of their delivery systems is of particular importance for improving the biopharmaceutical aspects of therapy. In this regard, substituted 1,2,3 - triazoles are of interest, as they are capable of binding to various enzymes and receptors, exhibiting high biological activity. Currently, 1,2,3-triazoles, as a class of N-heterocyclic compounds, due to their dual functionality, are used both as pharmacophores and linkers in molecular synthesis strategies. The paper presents the synthesis and properties of new chelates of europium and terbium ions with substituted 1,2,3-triazoles TR1 and TR2. Targeted synthesis of 1,2,3 - triazoles was carried out to increase solubility and improve complexation with lanthanide ions. 1,10-phenanthroline and 2,4-pentanedione were used as sensitizing chromophore ligands. The synthesized complexes exhibit high luminescent characteristics. Cellular cytotoxicity was studied for an individual ligand of 1,2,3 - triazole and terbium chelate. It is shown that bis-1,3-(4-methylcarboxyl-1,2,3-triazol-1-yl)benzene selectively acts on human duodenal adenocarcinoma cells, exhibiting high activity of 63.0 ± 4.7 μM. This compound is not toxic to human hepatocytes. The luminescent terbium complex [Tb(AcAc)3(TR2)] does not exhibit cytotoxicity in the studied cell lines and can be used as an optical probe without destructive effect on cells in vivo. Efficient solubilization of substituted 1,2,3-triazoles TR1 and TR2 and heteroligand complexes in the structure of the lyotropic mesophase Pluronic P123 / dimethylsulfoxide allows their use in biotic systems.
Keywords:
1,2,3-TRIAZOLE, HETEROLIGAND COMPLEXES OF LANTHANIDES, LUMINESCENCE, SOLUBILIZATION, LYOTROPIC MESOPHASES, PLURONIC P123, CYTOTOXICITY
1,2,3-TRIAZOLE, HETEROLIGAND COMPLEXES OF LANTHANIDES, LUMINESCENCE, SOLUBILIZATION, LYOTROPIC MESOPHASES, PLURONIC P123, CYTOTOXICITY
