Design and synthesis of gallocyanine inhibitors of DKK1/LRP6 interactions for treatment of Alzheimer's disease.

Savvas Thysiadis,Sotirios Katsamakas,Spyros Mpousis,Nicolaos Avramidis,Spiros Efthimiopoulos,Vasiliki Sarli

Bioorganic Chemistry（2018）

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摘要

•A series of NCI8642 derivatives was synthesized.•The synthesized NCI8642 derivatives inhibit DKK1/LRP6 interactions.•The synthesized NCI8642 derivatives inhibit Tau phosphorylation.•Alkylated NCI8642 derivatives on C1 provided the most active compounds.•The synthesized derivatives affect the levels of pGSK3β kinase and β-catenin.

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关键词

DKK1/LRP6 interactions,Tau phosphorylation,Phenoxazinone,Alzheimer’s disease,Gallocyanine derivatives

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