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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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    0357898 - ÚEB 2011 RIV AT eng J - Journal Article
    Gucký, Tomáš - Řezníčková, Eva - Džubák, P. - Hajdúch, M. - Kryštof, Vladimír
    Synthesis and anticancer activity of some 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines.
    Monatshefte fur Chemie. Roč. 141, č. 6 (2010), s. 709-714. ISSN 0026-9247. E-ISSN 1434-4475
    R&D Projects: GA ČR GA204/08/0511; GA ČR GA301/08/1649
    Institutional research plan: CEZ:AV0Z50380511
    Keywords : Pyrazolo[4,3-e][1,2,4]triazine * Anticancer * Cyclin-dependent kinase
    Subject RIV: EB - Genetics ; Molecular Biology
    Impact factor: 1.356, year: 2010

    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).
    Permanent Link: http://hdl.handle.net/11104/0006387

     
     
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