Keywords
1,2,3-triazoles
azide--alkyne cycloaddition
cancer cells
cell death
chemosensitizing effect
cisplatin
HDAC inhibitors
histone deacetylases
hydroxamic acids
Abstract
A new series of hydroxamic acids containing a 1,2,3-triazole moiety were obtained by the cycloaddition of methyl (2-azidoethoxy)acetate to a variety of acetylenes followed by treatment with hydroxylamine. The evaluation of their inhibitory activity against HDAC1, HDAC3, and HDAC8 revealed that N-hydroxy-2-[4-(4-pentylphenyl)-1H-1,2,3- triazol-1-yl]ethoxyacetamide showed the strongest HDAC inhibition and markedly enhanced cisplatin-induced apoptosis and antiproliferative effects in A431 cells, reducing the cisplatin IC50 from 15.64 ± 0.53 to 6.46 ± 0.87 μm (p < 0.05).
Funders
Russian Science Foundation
25-73-20033
References
1.
Neganova M.E., Klochkov S.G., Aleksandrova Y.R., Aliev G.
Current Medicinal Chemistry,
2020