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Synthesis and anticancer activity of some 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines

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Abstract

The deregulation of cell cycle components in cancer cells has provided a rationale for the development of small molecule inhibitors of cyclin-dependent kinases as novel anticancer drugs. A series of 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines was synthesized and their kinase inhibitory activity and cytotoxicity against several cancer cell lines has been evaluated. Some of the compounds of the series exhibited induction of caspase-dependent cell death and inhibition of cyclin-dependent kinase 2 (CDK2).

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Acknowledgments

We are grateful to grants MSM6198959216 from the Ministry of Education, Youth and Sports, 204/08/0511 and 301/08/1649 from the Czech Science Foundation and infrastructural project from EEA/Norway Financial Mechanisms (CZ0099).

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Authors and Affiliations

  1. Laboratory of Growth Regulators, Faculty of Science, Palacký University and Institute of Experimental Botany ASCR, Šlechtitelů 11, 78371, Olomouc, Czech Republic

    Tomáš Gucký, Eva Řezníčková & Vladimír Kryštof

  2. Laboratory of Experimental Medicine, Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacky University and Faculty Hospital in Olomouc, Olomouc, Czech Republic

    Petr Džubák & Marián Hajdúch

Authors
  1. Tomáš Gucký
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  2. Eva Řezníčková
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  3. Petr Džubák
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  4. Marián Hajdúch
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  5. Vladimír Kryštof
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Correspondence to Tomáš Gucký.

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Gucký, T., Řezníčková, E., Džubák, P. et al. Synthesis and anticancer activity of some 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines. Monatsh Chem 141, 709–714 (2010). https://doi.org/10.1007/s00706-010-0314-4

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  • DOI: https://doi.org/10.1007/s00706-010-0314-4

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