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Novel arylazopyrazole inhibitors of cyclin-dependent kinases

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    SYSNO ASEP0454915
    Document TypeJ - Journal Article
    R&D Document TypeJournal Article
    Subsidiary JČlánek ve WOS
    TitleNovel arylazopyrazole inhibitors of cyclin-dependent kinases
    Author(s) Jorda, Radek (UEB-Q) ORCID, RID
    Schütznerová, E. (CZ)
    Cankař, P. (CZ)
    Brychtová, Veronika (UEB-Q)
    Navrátilová, Jana (UEB-Q)
    Kryštof, Vladimír (UEB-Q) RID, ORCID
    Source TitleBioorganic & Medicinal Chemistry. - : Elsevier - ISSN 0968-0896
    Roč. 23, č. 9 (2015), s. 1975-1981
    Number of pages7 s.
    Languageeng - English
    CountryGB - United Kingdom
    KeywordsCyclin-dependent kinases ; Inhibitor ; Cell cycle
    Subject RIVCE - Biochemistry
    R&D ProjectsGAP305/12/0783 GA ČR - Czech Science Foundation (CSF)
    GA14-19590S GA ČR - Czech Science Foundation (CSF)
    LO1204 GA MŠk - Ministry of Education, Youth and Sports (MEYS)
    Institutional supportUEB-Q - RVO:61389030
    UT WOS000352698700007
    AnnotationHere, we describe new 4-arylazo-3,5-diamino-1H-pyrazole derivatives developed from CAN508, one of the first inhibitors to show preference for transcriptional regulator cyclin-dependent kinase 9. By substituting nitrogen in the pyrazole ring and employing a heteroatom in the 4-aryl ring, we obtained more potent derivatives differing in their CDK-selectivity profiles. The antiproliferative and anti-CDK kinase activities of the novel arylazopyrazoles were examined. The cellular effect of compound IVc was studied on MCF-7 cells synchronized by various methods and compared with other selective CDK inhibitors. The results demonstrated that IVc shows a preference for CDK4 and CDK1. In contrast to cytostatic effects induced by IVc in MCF-7 and K562 cells, we observed apoptotic activities in the RPMI-8226 cell line, which were confirmed by detecting active caspases by different biochemical assays.
    WorkplaceInstitute of Experimental Botany
    ContactDavid Klier,, Tel.: 220 390 469
    Year of Publishing2016
Number of the records: 1