Compounds > 2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1-3-4-oxadiazole

2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1-3-4-oxadiazole and Alzheimer-Disease

2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1-3-4-oxadiazole has been researched along with Alzheimer-Disease* in 1 studies

Other Studies

1 other study(ies) available for 2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1-3-4-oxadiazole and Alzheimer-Disease

Article	Year
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α. Journal of medicinal chemistry, 2012, May-10, Volume: 55, Issue:9 The glycogen synthase kinase-3 (GSK-3) has been linked to the pathogenesis of colorectal cancer, diabetes, cardiovascular disease, acute myeloid leukemia (AML), and Alzheimer's disease (AD). The debate on the respective contributions of GSK-3α and GSK-3β to AD pathology and AML is ongoing. Thus, the identification of potent GSK-3α-selective inhibitors, endowed with favorable pharmacokinetic properties, may elucidate the effect of GSK-3α inhibition in AD and AML models. The analysis of all available crystallized GSK-3 structures provided a simplified scheme of the relevant hot spots responsible for ligand binding and potency. This resulted in the identification of novel scorpion shaped GSK-3 inhibitors. It is noteworthy, compounds 14d and 15b showed the highest GSK-3α selectivity reported so far. In addition, compound 14d did not display significant inhibition of 48 out of 50 kinases in the test panel. The GSK-3 inhibitors were further profiled for efficacy and toxicity in the wild-type (wt) zebrafish embryo assay. Topics: Alzheimer Disease; Animals; Cell Line, Tumor; Cell Survival; Glycogen Synthase Kinase 3; Humans; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Mass Spectrometry; Models, Molecular; Molecular Dynamics Simulation; Oxadiazoles; Protein Kinase Inhibitors; Structure-Activity Relationship; Zebrafish	2012

Article

Year

Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α.

Journal of medicinal chemistry, 2012, May-10, Volume: 55, Issue:9

The glycogen synthase kinase-3 (GSK-3) has been linked to the pathogenesis of colorectal cancer, diabetes, cardiovascular disease, acute myeloid leukemia (AML), and Alzheimer's disease (AD). The debate on the respective contributions of GSK-3α and GSK-3β to AD pathology and AML is ongoing. Thus, the identification of potent GSK-3α-selective inhibitors, endowed with favorable pharmacokinetic properties, may elucidate the effect of GSK-3α inhibition in AD and AML models. The analysis of all available crystallized GSK-3 structures provided a simplified scheme of the relevant hot spots responsible for ligand binding and potency. This resulted in the identification of novel scorpion shaped GSK-3 inhibitors. It is noteworthy, compounds 14d and 15b showed the highest GSK-3α selectivity reported so far. In addition, compound 14d did not display significant inhibition of 48 out of 50 kinases in the test panel. The GSK-3 inhibitors were further profiled for efficacy and toxicity in the wild-type (wt) zebrafish embryo assay.

Topics: Alzheimer Disease; Animals; Cell Line, Tumor; Cell Survival; Glycogen Synthase Kinase 3; Humans; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Mass Spectrometry; Models, Molecular; Molecular Dynamics Simulation; Oxadiazoles; Protein Kinase Inhibitors; Structure-Activity Relationship; Zebrafish

2012