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.
| Identifer | oai:union.ndltd.org:DRESDEN/oai:qucosa:de:qucosa:87952 |
| Date | 09 November 2023 |
| Creators | Opitz, Ansgar, Seitz, Lisa-Marie, Krystof, Vladimir, Baselious, Fady, Holzer, Max, Sippl, Wolfgang, Hilgeroth, Andreas |
| Publisher | Future Science |
| Source Sets | Hochschulschriftenserver (HSSS) der SLUB Dresden |
| Language | English |
| Detected Language | English |
| Type | info:eu-repo/semantics/publishedVersion, doc-type:article, info:eu-repo/semantics/article, doc-type:Text |
| Rights | info:eu-repo/semantics/openAccess |
| Relation | 10.4155/fmc-2022-0061 |
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