5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).

No abstract is available for this paper.

• Publication year

  2003

• Venue

  Bioorganic & Medicinal Chemistry Letters

• Publication date

  2003-05-05

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/S0960-894X(03)00135-5PMID 12699760
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• 5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).

  2003cited by this paper
• Inhibition of glycogen synthase kinase 3 improves insulin action and glucose metabolism in human skeletal muscle.

  2002cited by this paper
• The Structure of Phosphorylated GSK-3β Complexed with a Peptide, FRATtide, that Inhibits β-Catenin Phosphorylation

  2001cited by this paper
• Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death.

  2001cited by this paper
• Specificity and mechanism of action of some commonly used protein kinase inhibitors.

  2000cited by this paper
• Expression, purification and crystallization of human tau-protein kinase I/glycogen synthase kinase-3beta.

  2000cited by this paper
• Specificity and mechanism of action of some commonly used protein kinase inhibitors

  2000cited by this paper
• Role of Glycogen Synthase Kinase-3 in the Phosphatidylinositol 3-Kinase/Akt Cell Survival Pathway*

  1998cited by this paper
• Expression and characterization of glycogen synthase kinase-3 mutants and their effect on glycogen synthase activity in intact cells.

  1996cited by this paper
• High-resolution crystal structures of human cyclin-dependent kinase 2 with and without ATP: bound waters and natural ligand as guides for inhibitor design.

  1996cited by this paper
• Multiple mechanisms for the phosphorylation of C-terminal regulatory sites in rabbit muscle glycogen synthase expressed in COS cells.

  1996cited by this paper
• A molecular mechanism for the effect of lithium on development.

  1996cited by this paper
• Alzheimer's disease-like phosphorylation of the microtubule-associated protein tau by glycogen synthase kinase-3 in transfected mammalian cells.

  1994cited by this paper
• Mechanisms of multisite phosphorylation and inactivation of rabbit muscle glycogen synthase.

  1993cited by this paper
• Pathogenesis of NIDDM: A Balanced Overview

  1992cited by this paper
• Insulin Resistance in Skeletal Muscles in Patients With NIDDM

  1992cited by this paper
• A common denominator linking glycogen metabolism, nuclear oncogenes and development.

  1991cited by this paper
• Intracellular glucose oxidation and glycogen synthase activity are reduced in non-insulin-dependent (type II) diabetes independent of impaired glucose uptake.

  1990cited by this paper
• Control of glycogen synthase by hierarchal protein phosphorylation

  1990cited by this paper
• Effects of insulin infusion on human skeletal muscle pyruvate dehydrogenase, phosphofructokinase, and glycogen synthase. Evidence for their role in oxidative and nonoxidative glucose metabolism.

  1987cited by this paper
• Correlation between muscle glycogen synthase activity and in vivo insulin action in man.

  1984cited by this paper
• Separation and characterisation of glycogen synthase kinase 3, glycogen synthase kinase 4 and glycogen synthase kinase 5 from rabbit skeletal muscle.

  1982cited by this paper
• Biosynthesis of glycogen from uridine diphosphate glucose.

  1959cited by this paper

• A Tetrazine‐Based Synthesis for Accessing Underutilized Aza‐Indole Analogues

  2025cites this paper
• Molecular Design, Synthesis and Anti-cancer Activity of Novel Pyrazolo[3,4-b]pyridine-based Glycohybrid Molecules.

  2025cites this paper
• Advances in targeting glycogen synthase kinase 3β for diabetes therapy.

  2025cites this paper
• Design, synthesis and anticancer evaluation of novel hydrazide-2-oxindole analogues as GSK-3β kinase inhibitors

  2025cites this paper
• New pyrazolopyridine and pyrazolothiazole-based compounds as anti-proliferative agents targeting c-Met kinase inhibition: design, synthesis, biological evaluation, and computational studies

  2023cites this paper
• Design, synthesis, and biological evaluation of furan-bearing pyrazolo[3,4-b]pyridines as novel inhibitors of CDK2 and P53-MDM2 protein-protein interaction.

  2023cites this paper
• Pyrazolopyridine: An efficient pharmacophore in recent drug design and development

  2022cites this paper
• One-pot three-component synthesis of novel pyrazolo[3,4-b]pyridines as potent antileukemic agents.

  2021cites this paper
• Design, Synthesis, and Biological Evaluation of Novel 7H-[1,2,4]Triazolo[3,4-b][1,3,4]thiadiazine Inhibitors as Antitumor Agents

  2020cites this paper
• A high throughput zebrafish chemical screen reveals ALK5 and non-canonical androgen signalling as modulators of the pkd2−/− phenotype

  2020cites this paper
• Competitive routes to cyclizations of polyfluoroalkyl-containing 2-tolylhydrazinylidene-1,3-diketones with 3-aminopyrazoles into bioactive pyrazoloazines

  2020cites this paper
• A multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer's disease.

  2019cites this paper
• Discovery and optimization of novel pyridines as highly potent and selective glycogen synthase kinase 3 inhibitors.

  2019cites this paper
• Serendipitous Formation of 2H-Pyrazolo[3,4-d]pyridazin-7(6H)-ones from 3-Arylsydnones

  2019cites this paper
• GSK3 suppression upregulates β-catenin and c-Myc to abrogate KRas-dependent tumors

  2018cites this paper
• Synthetic Fiber Dyeing with New Pyrazole Disperse Dyes and Their Colorimetric and Fastness Properties

  2018cites this paper
• Computer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3

  2018cites this paper
• Amaryllidaceae Alkaloids as Potential Glycogen Synthase Kinase-3β Inhibitors

  2018cites this paper
• Glycogen synthase kinase-3 and its inhibitors: Potential target for various therapeutic conditions.

  2018cites this paper
• Synthesis of new heterocyclic compounds based on pyrazolopyridine scaffold and evaluation of their neuroprotective potential in MPP+-induced neurodegeneration.

  2017cites this paper
• Meglumine catalyzed one-pot green synthesis of novel 4,7-dihydro-1H-pyrazolo[3,4-b]pyridin-6-amines

  2017cites this paper
• Novel and convenient one-pot strategy for regioselective synthesis of new 5-aryl-3-methyl-1-phenyl-1,2-dihydro-7aH-pyrazolo[3,4-c]pyridazin-7a-ol derivatives

  2017cites this paper
• Comprehensive characterization of the Published Kinase Inhibitor Set

  2016cites this paper
• Synthesis and biological evaluation of some functionalized 1H-1,2,3-triazole tethered pyrazolo[3,4-b]pyridin-6(7H)-ones as antimicrobial and apoptosis inducing agents

  2016cites this paper
• Down regulation of Chk1 by p53 plays a role in synergistic induction of apoptosis by chemotherapeutics and inhibitors for Jak2 or BCR/ABL in hematopoietic cells

  2016cites this paper
• Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.

  2016cites this paper
• Hit Optimization of 5-Substituted-N-(piperidin-4-ylmethyl)-1H-indazole-3-carboxamides: Potent Glycogen Synthase Kinase-3 (GSK-3) Inhibitors with in Vivo Activity in Model of Mood Disorders.

  2015cites this paper
• Utility of 3-amino-1H-pyrazolo[3,4-c]pyridazine in heterocyclic synthesis

  2015cites this paper
• Synthesis, Reactions, and Pharmacological Evaluations of Some Novel Pyridazolopyridiazine Candidates

  2014cites this paper
• The anticancer potential of various substituted pyridazines and related compounds

  2014cites this paper
• Quantitative Structure‐Activity Relationship Analysis and a Combined Ligand‐Based/Structure‐Based Virtual Screening Study for Glycogen Synthase Kinase‐3

  2014cites this paper
• Profile of the GSK Published Protein Kinase Inhibitor Set Across ATP-Dependent and-Independent Luciferases: Implications for Reporter-Gene Assays

  2013cites this paper
• Inhibition of the PI3K/Akt/GSK3 Pathway Downstream of BCR/ABL, Jak2-V617F, or FLT3-ITD Downregulates DNA Damage-Induced Chk1 Activation as Well as G2/M Arrest and Prominently Enhances Induction of Apoptosis

  2013cites this paper
• Exploration of antimicrobial potential of pyrazolo[3,4-b]pyridine scaffold bearing benzenesulfonamide and trifluoromethyl moieties

  2013cites this paper
• Synthesis and antiviral evalution of some novel pyrazoles and pyrazolo[3,4-d]pyridazines bearing 5,6,7,8-tetrahydronaphthalene.

  2013cites this paper
• Identification of Autophosphorylation Inhibitors of the Inositol-Requiring Enzyme 1 Alpha (IRE1α) by High-Throughput Screening Using a DELFIA Assay

  2013cites this paper
• Pharmacological activities evaluation of some new pyrazolo-pyrimidino-pyridazine derivatives

  2013cites this paper
• DESIGN, SYNTHESIS, BIOLOGICAL EVALUATION AND MOLECULAR DOCKING STUDIES OF NOVEL QUINAZOLINE DERIVATIVES AS GSK-3B INHIBITORS

  2013cites this paper
• 6-(4-Pyridyl)pyrimidin-4(3H)-ones as CNS penetrant glycogen synthase kinase-3β inhibitors.

  2013cites this paper
• Small-Molecule Inhibitors of GSK-3: Structural Insights and Their Application to Alzheimer's Disease Models

  2012cites this paper
• Discovery of Novel Glycogen Synthase Kinase-3beta Inhibitors: Molecular Modeling, Virtual Screening, and Biological Evaluation

  2012cites this paper
• Glycogen synthase kinase 3 as an anticancer drug target: novel experimental findings and trends in the design of inhibitors.

  2012cites this paper
• Synthesis of Novel Bis-enaminones by KHSO4-assisted Facile Michael Addition-elimination Reaction of 3-(dimethylamino)-1-phenylprop-2-en-1-ones with Diamines in Water

  2011cites this paper
• Binding Studies and Quantitative Structure–Activity Relationship of 3‐Amino‐1H‐Indazoles as Inhibitors of GSK3β

  2011cites this paper
• Structure‐Based Virtual Screening of Glycogen Synthase Kinase 3β Inhibitors: Analysis of Scoring Functions Applied to Large True Actives and Decoy Sets

  2011cites this paper
• DNA Damage Stress and Inhibition of Jak2-V617F Cause Its Degradation and Synergistically Induce Apoptosis through Activation of GSK3β

  2011influential citation
• Substrate competitive GSK-3 inhibitors - strategy and implications.

  2010cites this paper
• Synthesis and characterization of some pyrazole derivatives of 1,5‐diphenyl‐1H‐pyrazole‐3,4‐dicarboxylic acid

  2010cites this paper
• Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.

  2010cites this paper
• Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.

  2010cites this paper
• Ionic liquid-promoted multi-component reaction: novel and efficient preparation of pyrazolo[3,4-b]pyridinone, pyrazolo[3,4-b]-quinolinone and their hybrids with pyrimidine nucleoside

  2010cites this paper
• Pyridazine derivatives and related compounds. 23*. Synthesis of 3-substituted pyrazolo[3,4-c]pyridazines and their application as disperse dyes

  2010cites this paper
• Radioiodination of 3-iodo-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazine via isotopic exchange reaction

  2010cites this paper
• Studies on the acetylation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile derivatives

  2010cites this paper
• GSK3 inhibitors and disease.

  2009cites this paper
• Glycogen synthase kinase-3 inhibition by 3-anilino-4-phenylmaleimides: insights from 3D-QSAR and docking

  2009cites this paper
• Selective enzyme inhibition in the prevention of neuronal apoptosis : a molecular modelling study

  2009cites this paper
• 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.

  2009cites this paper
• GSK-3 Inhibitors: A Ray of Hope for the Treatment of Alzheimer's Disease?

  2008cites this paper
• Selectivity criterion for pyrazolo[3,4-b]pyrid[az]ine derivatives as GSK-3 inhibitors: CoMFA and molecular docking studies.

  2008cites this paper
• Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin.

  2008cites this paper
• Synthesis of pyrazolo[3,4‐b]pyridines and attachment of amino acids and carbohydrate as linkers

  2008cites this paper
• A Green Approach to the Synthesis of Biologically Important Indeno[2,1‐e]pyrazolo[5,4‐b]pyridines via Microwave‐assisted Multi‐component Reactions in Water

  2008cites this paper
• Efficient mono- and bis-functionalization of 3,6-dichloropyridazine using (tmp)2Zn.2MgCl2.2LiCl.

  2008cites this paper
• Preclinical efficacy on GSK‐3 inhibitors: Towards a future generation of powerful drugs

  2008cites this paper
• Increased expression of the WNT antagonist sFRP-1 in glaucoma elevates intraocular pressure.

  2008cites this paper
• Novel GSK-3beta inhibitors from sequential virtual screening.

  2008cites this paper
• Bicyclic 5-6 Systems: Other Four Heteroatoms 2:2

  2008cites this paper
• Bicyclic 5-6 Systems: Three Heteroatoms 2:1

  2008cites this paper
• Novel GSK-3β inhibitors from sequential virtual screening

  2008cites this paper
• Chapter 6.3 Triazines, tetrazines and fused ring polyaza systems

  2008cites this paper
• A novel reaction of the "Huisgen zwitterion" with chalcones and dienones: an efficient strategy for the synthesis of pyrazoline and pyrazolopyridazine derivatives.

  2007cites this paper
• Pharmacological modulation of stem cell function.

  2007cites this paper
• 3D QSAR Methods: Phase and Catalyst Compared

  2007cites this paper
• An efficient synthesis of new class of pyrazolo[3,4‐b]pyridine‐6‐one derivatives by a novel cascade reaction

  2007cites this paper
• QSAR studies for the pharmacological inhibition of glycogen synthase kinase-3.

  2007cites this paper
• Identification of potential glycogen kinase-3 inhibitors by structure based virtual screening.

  2007cites this paper
• Tau therapeutic strategies for the treatment of Alzheimer's disease.

  2006cites this paper
• Synthesis and in vitro antitumor evaluation of some indeno[1,2-c]pyrazol(in)es substituted with sulfonamide, sulfonylurea(-thiourea) pharmacophores, and some derived thiazole ring systems.

  2006cites this paper
• QSAR modeling of the inhibition of glycogen synthase kinase-3.

  2006cites this paper
• Probing the physicochemical and structural requirements for glycogen synthase kinase-3alpha inhibition: 2D-QSAR for 3-anilino-4-phenylmaleimides.

  2006cites this paper
• De novo and molecular target-independent discovery of orally bioavailable lead compounds for neurological disorders.

  2006cites this paper
• Investigation of Potential Glycogen Synthase Kinase 3 Inhibitors Using Pharmacophore Mapping and Virtual Screening

  2006cites this paper
• Regioselective functionalization of trisubstituted pyridines using a bromine-magnesium exchange.

  2006cites this paper
• Emerging targets for diabetes

  2005cites this paper
• Pyrazolo[3,4-c]pyridazines as novel and selective inhibitors of cyclin-dependent kinases.

  2005cites this paper
• The role of hydrophobic properties of chemicals in promoting allosteric reactions.

  2005cites this paper
• GSK-3 inhibitors and their potential in the treatment of Alzheimer’s disease

  2005cites this paper
• Development of glucose intolerance in male transgenic mice overexpressing human glycogen synthase kinase-3beta on a muscle-specific promoter.

  2004cites this paper
• The design of drug candidate molecules as selective inhibitors of therapeutically relevant protein kinases.

  2004cites this paper
• N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.

  2004cites this paper
• Intervention of hepatic glucose production. Small molecule regulators of potential targets for Type 2 diabetes therapy.

  2004cites this paper
• 4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors.

  2004cites this paper
• GSK-3 inhibitors: discoveries and developments.

  2004cites this paper
• Discovery and development of GSK3 inhibitors for the treatment of type 2 diabetes.

  2004cites this paper
• 3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.

  2004cites this paper
• Pharmacological inhibitors of glycogen synthase kinase 3.

  2004influential citation
• Challenges and opportunities with glycogen synthase kinase-3 inhibitors for insulin resistance and Type 2 diabetes treatment

  2003influential citation
• 6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).

  2003cites this paper
• CDK versus GSK-3 inhibition: a purple haze no longer?

  2003cites this paper