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

作者：Thysiadis Savvas; Mpousis Spyros; Avramidis Nicolaos; Katsamakas Sotirios; Balomenos Athanasios; Remelli Rosaria; Efthimiopoulos Spyros^*; Sarli Vasiliki^*

来源：Bioorganic & Medicinal Chemistry, 2016, 24(5): 1014-1022.

DOI：10.1016/j.bmc.2016.01.025

• DKK1/LRP6 interaction inhibitors
• Phenoxazinone
• Tau phosphorylation inhibitors
• NCI8642
• Wnt signaling

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 beta-catenin, and decrease the DKK1-induced Tau phosphorylation at serine 396.

• 出版日期2016-3-1