Novel arylazopyrazole inhibitors of cyclin-dependent kinases

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F15%3A33157437" target="_blank" >RIV/61989592:15310/15:33157437 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61389030:_____/15:00454915 RIV/00209805:_____/15:#0000611

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0968089615002096" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0968089615002096</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.bmc.2015.03.025" target="_blank" >10.1016/j.bmc.2015.03.025</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Novel arylazopyrazole inhibitors of cyclin-dependent kinases

Popis výsledku v původním jazyce

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 employinga 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.

Název v anglickém jazyce

Novel arylazopyrazole inhibitors of cyclin-dependent kinases

Popis výsledku anglicky

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 employinga 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.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2015

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Bioorganic &amp; Medicinal Chemistry

ISSN

0968-0896

e-ISSN

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Svazek periodika

23

Číslo periodika v rámci svazku

9

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

7

Strana od-do

1975-1981

Kód UT WoS článku

000352698700007

EID výsledku v databázi Scopus

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