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. 2016 Mar 1;24(5):1014-22.
doi: 10.1016/j.bmc.2016.01.025. Epub 2016 Jan 16.

Discovery of novel phenoxazinone derivatives as DKK1/LRP6 interaction inhibitors: Synthesis, biological evaluation and structure-activity relationships

Savvas Thysiadis  1 , Spyros Mpousis  1 , Nicolaos Avramidis  2 , Sotirios Katsamakas  3 , Athanasios Balomenos  2 , Rosaria Remelli  4 , Spyros Efthimiopoulos  2 , Vasiliki Sarli  1
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Discovery of novel phenoxazinone derivatives as DKK1/LRP6 interaction inhibitors: Synthesis, biological evaluation and structure-activity relationships

Savvas Thysiadis et al. Bioorg Med Chem. .

Abstract

Amino derivatives of NCI8642 were synthesized and evaluated as inhibitors of DKK1/LRP6 interactions. The new inhibitors were able to activate the Wnt signaling pathway as indicated by the increased levels of β-catenin, and decrease the DKK1-induced Tau phosphorylation at serine 396.

Keywords: DKK1/LRP6 interaction inhibitors; NCI8642; Phenoxazinone; Tau phosphorylation inhibitors; Wnt signaling.

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