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Synthesis and Cytotoxic Activity of Fluorine-Containing 6,7-Dihydroindazolone and 6,7-Dihydrobenzisoxazolone Derivatives

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The oximes of fluorine-containing 6,7-dihydroindazole-4,5-diones and 6,7-dihydrobenzisoxazole-4-5-diones, 5-[3-fluorobenzoyloxy)imino)]-6,6-dimethyl-3-(3-fluorophenyl)-6,7-dihydrobenz[d]]isoxazol-4(5H)-one, and 5,5-dimethyl-7-phenyl-9-(4-fluorophenyl)-3,5,6,7-tetrahydro-2H-pyrazolo[4,3-f]quinoxaline were synthesized. The cytotoxic activity of these compounds against cell lines MCF-7 (human breast carcinoma) and HepG2 (human hepatocellular carcinoma) was determined. The fluorine-containing 6,7-dihydroindazolone derivatives synthesized here included substances with marked antiproliferative activity, the mechanism of which may be linked with induction of apoptosis due to impairment of the regular cell cycle, i.e., delayed of tumor cells in the G2/M phase.

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Correspondence to T. S. Khlebnikova.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 7, pp. 21 – 26, July, 2020.

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Khlebnikova, T.S., Piven’, Y.A., Zinovich, V.G. et al. Synthesis and Cytotoxic Activity of Fluorine-Containing 6,7-Dihydroindazolone and 6,7-Dihydrobenzisoxazolone Derivatives. Pharm Chem J 54, 700–706 (2020). https://doi.org/10.1007/s11094-020-02258-z

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  • DOI: https://doi.org/10.1007/s11094-020-02258-z

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