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

[Display omitted] 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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2016-03, Vol.24 (5), p.1014-1022
Hauptverfasser:	Thysiadis, Savvas, Mpousis, Spyros, Avramidis, Nicolaos, Katsamakas, Sotirios, Balomenos, Athanasios, Remelli, Rosaria, Efthimiopoulos, Spyros, Sarli, Vasiliki
Format:	Artikel
Sprache:	eng
Schlagworte:	beta Catenin - metabolism DKK1/LRP6 interaction inhibitors HEK293 Cells Humans Intercellular Signaling Peptides and Proteins - metabolism Low Density Lipoprotein Receptor-Related Protein-6 - metabolism Models, Molecular NCI8642 Oxazines - chemical synthesis Oxazines - chemistry Oxazines - pharmacology Phenoxazinone Phosphorylation - drug effects Protein Interaction Maps - drug effects Signal Transduction - drug effects Structure-Activity Relationship Tau phosphorylation inhibitors Wnt Proteins - metabolism Wnt signaling
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Zusammenfassung:	[Display omitted] 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.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2016.01.025