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

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• 作者：Savvas Thysiadis^a ; Spyros Mpousis^a ; Nicolaos Avramidis^b ; Sotirios Katsamakas^c ; Athanasios Balomenos^b ; Rosaria Remelli^d ; Spyros Efthimiopoulos^b ; ; Vasiliki Sarli^a ;
• 关键词：DKK1/LRP6 interaction inhibitors ; Phenoxazinone ; Tau phosphorylation inhibitors ; NCI8642 ; Wnt signaling
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：1 March 2016
• 年：2016
• 卷：24
• 期：5
• 页码：1014-1022
• 全文大小：1372 K

文摘

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.