Novel effective small-molecule inhibitors of protein kinases related to tau pathology in Alzheimer's disease
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F22%3A73616105" target="_blank" >RIV/61989592:15310/22:73616105 - isvavai.cz</a>
Result on the web
<a href="https://obd.upol.cz/id_publ/333195992" target="_blank" >https://obd.upol.cz/id_publ/333195992</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.4155/fmc-2022-0061" target="_blank" >10.4155/fmc-2022-0061</a>
Alternative languages
Result language
angličtina
Original language name
Novel effective small-molecule inhibitors of protein kinases related to tau pathology in Alzheimer's disease
Original language description
Alzheimer's disease (AD) drugs in therapy are limited to acetylcholine esterase inhibitors and memantine. Newly developed drugs against a single target structure have an insufficient effect on symptomatic AD patients. Results: Novel aromatically anellated pyridofuranes have been evaluated for inhibition of AD-relevant protein kinases cdk1, cdk2, gsk-3b and Fyn. Best activities have been found for naphthopyridofuranes with a hydroxyl function as part of the 5-substituent and a hydrogen or halogen substituent in the 8-position. Best results in nanomolar ranges were found for benzopyridofuranes with a 6-hydroxy and a 3-alkoxy substitution or an exclusive 6-alkoxy substituent. Conclusion: First lead compounds were identified inhibiting two to three kinases in nanomolar ranges to be qualified as an innovative approach for AD multitargeting.
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
30107 - Medicinal chemistry
Result continuities
Project
<a href="/en/project/EF16_019%2F0000868" target="_blank" >EF16_019/0000868: Molecular, cellular and clinical approach to healthy ageing</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Future Medicinal Chemistry
ISSN
1756-8919
e-ISSN
1756-8927
Volume of the periodical
14
Issue of the periodical within the volume
16
Country of publishing house
GB - UNITED KINGDOM
Number of pages
12
Pages from-to
1175-1186
UT code for WoS article
000835345100001
EID of the result in the Scopus database
2-s2.0-85136342812