Trisubstituted Pyrazolopyrimidines as Novel Angiogenesis Inhibitors
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F13%3A33148299" target="_blank" >RIV/61989592:15310/13:33148299 - isvavai.cz</a>
Alternative codes found
RIV/61389030:_____/13:00395043
Result on the web
<a href="http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0054607" target="_blank" >http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0054607</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1371/journal.pone.0054607" target="_blank" >10.1371/journal.pone.0054607</a>
Alternative languages
Result language
angličtina
Original language name
Trisubstituted Pyrazolopyrimidines as Novel Angiogenesis Inhibitors
Original language description
Current inhibitors of angiogenesis comprise either therapeutic antibodies (e.g. bevacicumab binding to VEGF-A) or small molecular inhibitors of receptor tyrosin kinases like e.g. sunitinib, which inhibits PDGFR and VEGFR. We have recently identified cyclin-dependent kinase 5 (Cdk5) as novel alternative and pharmacologically accessible target in the context of angiogenesis. In the present work we demonstrate that trisubstituted pyrazolo[4,3-d]pyrimidines constitute a novel class of compounds which potently inhibit angiogenesis. All seven tested compounds inhibited endothelial cell proliferation with IC50 values between 1 and 18 mu M. Interestingly, this seems not to be due to cytotoxicity, since none of them showed acute cytotoxic effects on endothelialcells at a concentration of 10 mu M,. The three most potent compounds (LGR1404, LGR1406 and LGR1407) also inhibited cell migration (by 27, 51 and 31%, resp.), chemotaxis (by 50, 70 and 60% in accumulative distance, resp.), and tube forma
Czech name
—
Czech description
—
Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
ED - Physiology
OECD FORD branch
—
Result continuities
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)
Others
Publication year
2013
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
PLoS One
ISSN
1932-6203
e-ISSN
—
Volume of the periodical
8
Issue of the periodical within the volume
1
Country of publishing house
US - UNITED STATES
Number of pages
12
Pages from-to
"e54607"
UT code for WoS article
000314707700068
EID of the result in the Scopus database
—