Τίτλος:
Discovery of novel phenoxazinone derivatives as DKK1/LRP6 interaction inhibitors: Synthesis, biological evaluation and structure-activity relationships
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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. © 2016 Elsevier Ltd. All rights reserved.
Συγγραφείς:
Thysiadis, S.
Mpousis, S.
Avramidis, N.
Katsamakas, S.
Balomenos, A.
Remelli, R.
Efthimiopoulos, S.
Sarli, V.
Περιοδικό:
BIOORGANIC AND MEDICINAL CHEMISTRY
Εκδότης:
Elsevier Ireland Ltd
Λέξεις-κλειδιά:
beta catenin; butyl 7 (dimethylamino) 4 hydroxy 2 [(4 methoxybenzyl) amino] 3 oxo 3h phenoxazine 1 carboxylate; dickkopf 1 protein; gallocyanine; gallocyanine derivative; low density lipoprotein receptor related protein 6; methyl 2 (cyclohexylamino) 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate; methyl 2 (cyclopentylamino) 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate; methyl 2 amino 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate; methyl 2 [(3,4 dichlorophenyl)amino] 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate; methyl 7 (dimethylamino) 4 hydroxy 2 morpholino 3 oxo 3h phenoxazine 1 carboxylate; methyl 7 (dimethylamino) 4 hydroxy 2 [(4 methoxybenzyl) amino] 3 oxo 3h phenoxazine 1 carboxylate; methyl 7 (dimethylamino) 4 hydroxy 2 [(4 methoxyphenyl) amino] 3 oxo 3h phenoxazine 1 carboxylate; methyl 7 (dimethylamino) 4 hydroxy 3 oxo 2 (2 tolyl amino) 3h phenoxazine 1 carboxylate; methyl 7 (dimethylamino) 4 hydroxy 3 oxo 2 (phenylamino) 3h phenoxazine 1 carboxylate; methyl 7 (dimethylamino) 4 hydroxy 3 oxo 2 (piperidin 1 yl) 3h phenoxazine 1 carboxylate; phenoxazinone derivative; protein inhibitor; serine; tau protein; unclassified drug; Wnt protein; DKK1 protein, human; low density lipoprotein receptor related protein 6; LRP6 protein, human; oxazine derivative; phenoxazinone; signal peptide, Article; controlled study; cytotoxicity; drug screening; drug synthesis; human; human cell; protein phosphorylation; signal transduction; structure activity relation; chemistry; drug effects; HEK293 cell line; metabolism; molecular model; phosphorylation; protein protein interaction; structure activity relation; synthesis, beta Catenin; HEK293 Cells; Humans; Intercellular Signaling Peptides and Proteins; Low Density Lipoprotein Receptor-Related Protein-6; Models, Molecular; Oxazines; Phosphorylation; Protein Interaction Maps; Signal Transduction; Structure-Activity Relationship; Wnt Proteins
DOI:
10.1016/j.bmc.2016.01.025
