TY - JOUR
TI - Synthesis and evaluation of gallocyanine dyes as potential agents for the treatment of Alzheimer's disease and related neurodegenerative tauopathies
AU - Mpousis, S.
AU - Thysiadis, S.
AU - Avramidis, N.
AU - Katsamakas, S.
AU - Efthimiopoulos, S.
AU - Sarli, V.
JO - European Journal of Medicinal Chemistry
PY - 2016
VL - 108
TODO - null
SP - 28-38
PB - Elsevier Masson SAS
SN - 0223-5234
TODO - 10.1016/j.ejmech.2015.11.024
TODO - 2 methoxyethyl 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  7 (dimethylamino) 1 hydroxy 3h phenoxazin 3 one;  7 (dimethylamino) 1 methyl 3h phenoxazine 3 one;  7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  7 (dimethylamino) 4 hydroxy 3h phenoxazin 3 one;  benzyl 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  butyl 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  butyl 7 (dipropylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  cyanine dye;  dickkopf 1 protein;  ethyl 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  gallocyanine dye;  hexyl 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  isopropyl 7 (dimethylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  low density lipoprotein receptor related protein;  methyl 7 (dipropylamino) 4 hydroxy 3 oxo 3h phenoxazine 1 carboxylate;  n [6,7 dihydroxy 9 [(2 methoxyethoxy)carbonyl] 3h phenoxazin 3 ylidene] n methymethanaminium chloride;  n [9 (butoxycarbonyl) 6,7 dihydroxy 3h phenoxazin 3 ylidene] n methylmethanamin chloride;  n [9 (ethoxycarbonyl) 6,7 dihydroxy 3h phenoxazin 3 ylidene] n methylmethanamin chloride;  n [9 [(hexyloxy)carbonyl] 6,7 dihydroxy 3h phenoxazin 3 ylidene] n methylmethan aminium chloride;  nootropic agent;  prostaglandin J2;  tau protein;  unclassified drug;  coloring agent;  DKK1 protein, human;  gallocyanine;  low density lipoprotein receptor related protein;  oxazine derivative;  protein binding;  signal peptide;  tau protein, Alzheimer disease;  animal cell;  Article;  cell culture;  cytolysis;  drug potency;  drug screening;  drug synthesis;  embryo;  HEK293 cell line;  human;  human cell;  mouse;  nonhuman;  protein phosphorylation;  protein protein interaction;  surface plasmon resonance;  tauopathy;  Western blotting;  Wnt signaling pathway;  Alzheimer disease;  chemical structure;  chemistry;  dose response;  drug effects;  metabolism;  molecular model;  phosphorylation;  structure activity relation;  synthesis;  Tauopathies, Alzheimer Disease;  Coloring Agents;  Dose-Response Relationship, Drug;  Humans;  Intercellular Signaling Peptides and Proteins;  Low Density Lipoprotein Receptor-Related Protein-1;  Models, Molecular;  Molecular Structure;  Oxazines;  Phosphorylation;  Protein Binding;  Structure-Activity Relationship;  tau Proteins;  Tauopathies
TODO - In search of safe and effective anti-Alzheimer disease agents a series of gallocyanine dyes have been synthesized and evaluated for their ability to inhibit LRPs/DKK1 interactions. Modulation of the interactions between LRPS and DKK1, regulate Wnt signaling pathway and affect Tau phosphorylation. The current efforts resulted in the identification of potent DKK1 inhibitors which are able to inhibit prostaglandin J2-induced tau phosphorylation at serine 396. © 2015 Elsevier Masson SAS.
ER -