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Novel arylazopyrazole inhibitors of cyclin-dependent kinases

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    SYSNO ASEP0454915
    Druh ASEPJ - Článek v odborném periodiku
    Zařazení RIVJ - Článek v odborném periodiku
    Poddruh JČlánek ve WOS
    NázevNovel arylazopyrazole inhibitors of cyclin-dependent kinases
    Tvůrce(i) 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
    Zdroj.dok.Bioorganic & Medicinal Chemistry. - : Elsevier - ISSN 0968-0896
    Roč. 23, č. 9 (2015), s. 1975-1981
    Poč.str.7 s.
    Jazyk dok.eng - angličtina
    Země vyd.GB - Velká Británie
    Klíč. slovaCyclin-dependent kinases ; Inhibitor ; Cell cycle
    Vědní obor RIVCE - Biochemie
    CEPGAP305/12/0783 GA ČR - Grantová agentura ČR
    GA14-19590S GA ČR - Grantová agentura ČR
    LO1204 GA MŠk - Ministerstvo školství, mládeže a tělovýchovy
    Institucionální podporaUEB-Q - RVO:61389030
    UT WOS000352698700007
    DOI10.1016/j.bmc.2015.03.025
    AnotaceHere, 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.
    PracovištěÚstav experimentální botaniky
    KontaktDavid Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469
    Rok sběru2016
Počet záznamů: 1