The cytotoxic activity of perfluoroalkyl imidazoindazoles and imidazobenzisoxazoles with respect to MCF-7 (human breast carcinoma) and HepG2 cell lines (human hepatocellular carcinoma) was studied. The imidazoindazoles exhibited significant cytotoxicity against MCF-7 and HepG2 cell lines. 2,6-bis(4-Fluorophenyl)-4,4-dimethyl-8-trifluoromethyl-3,4,5,6-tetrahydroimidazo[4,5-e]indazole displayed the most pronounced cytotoxic action. Regioisomeric imidazobenzisoxazoles inhibited extensively growth of HepG2 cells. The mechanism of cytotoxic action can be related to the induction of apoptosis as a result of disruption of the cell cycle, in particular, arrest of HepG2 cells in the G2 phase and MCF-7 cells in the G1 phase.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 55, No. 3, pp. 10 – 14, March, 2021.
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Khlebnikova, T.S., Panibrat, O.V., Piven, Y.A. et al. Cytotoxic Activity of Perfluoroalkyl-Substituted Imidazoindazoles and Imidazobenzisoxazoles. Pharm Chem J 55, 219–223 (2021). https://doi.org/10.1007/s11094-021-02401-4
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DOI: https://doi.org/10.1007/s11094-021-02401-4