Pyrimidine-based pyrazoles as cyclin-dependent kinase 2 inhibitors: Design, synthesis, and biological evaluation
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F18%3A00493391" target="_blank" >RIV/61388963:_____/18:00493391 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1111/cbdd.13334" target="_blank" >http://dx.doi.org/10.1111/cbdd.13334</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1111/cbdd.13334" target="_blank" >10.1111/cbdd.13334</a>
Alternative languages
Result language
angličtina
Original language name
Pyrimidine-based pyrazoles as cyclin-dependent kinase 2 inhibitors: Design, synthesis, and biological evaluation
Original language description
A series of new pyrimidine-pyrazole hybrid molecules were designed as inhibitors of cyclin-dependent kinase 2. Designed compounds were docked using Glide and the compounds showing good score values and encouraging interactions with the residues were selected for synthesis. They were then evaluated using CDK2-CyclinA2 enzyme inhibition by a luminescent ADP detection assay. We show that of the 26 compounds synthesized and evaluated, at least 5 compounds were found to be highly potent (IC50<20nm), which can be further optimized to have selectivity over other kinase isoforms.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10403 - Physical chemistry
Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2018
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Chemical Biology & Drug Design
ISSN
1747-0277
e-ISSN
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Volume of the periodical
92
Issue of the periodical within the volume
3
Country of publishing house
GB - UNITED KINGDOM
Number of pages
9
Pages from-to
1683-1691
UT code for WoS article
000443302700010
EID of the result in the Scopus database
2-s2.0-85052550577