Počet záznamů: 1
Novel arylazopyrazole inhibitors of cyclin-dependent kinases
- 1.0454915 - ÚEB 2016 RIV GB eng J - Článek v odborném periodiku
Jorda, Radek - Schütznerová, E. - Cankař, P. - Brychtová, Veronika - Navrátilová, Jana - Kryštof, Vladimír
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
Bioorganic & Medicinal Chemistry. Roč. 23, č. 9 (2015), s. 1975-1981. ISSN 0968-0896
Grant CEP: GA ČR GAP305/12/0783; GA ČR GA14-19590S; GA MŠk(CZ) LO1204
Institucionální podpora: RVO:61389030
Klíčová slova: Cyclin-dependent kinases * Inhibitor * Cell cycle
Kód oboru RIV: CE - Biochemie
Impakt faktor: 2.923, rok: 2015
Here, 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.
Trvalý link: http://hdl.handle.net/11104/0255588
Název souboru Staženo Velikost Komentář Verze Přístup 2015_Jorda_BIOORGANIC & MEDICINAL CHEMISTRY_1975.pdf 3 1.3 MB Jiná povolen
Počet záznamů: 1