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- W4289544540 abstract "Background: 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." @default.
- W4289544540 created "2022-08-03" @default.
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- W4289544540 date "2022-08-01" @default.
- W4289544540 modified "2023-10-16" @default.
- W4289544540 title "Novel effective small-molecule inhibitors of protein kinases related to tau pathology in Alzheimer's disease" @default.
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- W4289544540 doi "https://doi.org/10.4155/fmc-2022-0061" @default.
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