Novel arylazopyrazole inhibitors of cyclin-dependent kinases

Result code in 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>

Alternative codes found

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

Result on the web

<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>

Result language

angličtina

Original language name

Novel arylazopyrazole inhibitors of cyclin-dependent kinases

Original language description

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.

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

CE - Biochemistry

OECD FORD branch

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Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

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

Publication year

2015

Confidentiality

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

Name of the periodical

Bioorganic &amp; Medicinal Chemistry

ISSN

0968-0896

e-ISSN

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Volume of the periodical

23

Issue of the periodical within the volume

9

Country of publishing house

GB - UNITED KINGDOM

Number of pages

7

Pages from-to

1975-1981

UT code for WoS article

000352698700007

EID of the result in the Scopus database

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