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Novel arylazopyrazole inhibitors of cyclin-dependent kinases

SYSNO ASEP	0454915
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	Novel 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 Title	Bioorganic & Medicinal Chemistry. - : Elsevier - ISSN 0968-0896 Roč. 23, č. 9 (2015), s. 1975-1981
Number of pages	7 s.
Language	eng - English
Country	GB - United Kingdom
Keywords	Cyclin-dependent kinases ; Inhibitor ; Cell cycle
Subject RIV	CE - Biochemistry
R&D Projects	GAP305/12/0783 GA ČR - Czech Science Foundation (CSF)
	GA14-19590S GA ČR - Czech Science Foundation (CSF)
	LO1204 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
Institutional support	UEB-Q - RVO:61389030
UT WOS	000352698700007
DOI	10.1016/j.bmc.2015.03.025
Annotation	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.
Workplace	Institute of Experimental Botany
Contact	David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469
Year of Publishing	2016

Number of the records: 1