Zeolite-catalyzed synthesis of pyrazolo[1,2- a ][1,2,4]triazole-1,3-dione derivatives as anti-breast cancer agents

2018 
A series of pyrazolo[1,2-a][1,2,4]triazole-1,3-dione derivatives were synthesized under the catalytic effect of Natrolite zeolite, and their cytotoxic effects on three human breast cancer cell lines viz. breast cancer (BT-474), triple negative breast cancer (MDA-MB 231), and breast carcinoma (MCF-7) were explored using MTT assay. Apoptotic effects of the compounds were investigated by western blot analysis on the caspase-3 protein. Moreover, we examined the level of reactive oxygen species in all three cell lines. The most promising compound, 7-Amino-1,3-dioxo-5-(4-nitrophenyl)-2-phenyl-1,2,3-trihydropyrazolo[1,2-a][1,2,4]triazole-6-carbonitrile (4c), showed high levels of cytotoxicity against all cell lines with IC50 values of 2.3, 2.5 and 3 μg/ml, respectively.
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