144 articles for thisTarget
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Article Title
Organization
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors.
Cnrs
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
University Of Nebraska Medical Center
Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.
Universit£
Novel optimization of valmerins (tetrahydropyrido[1,2-a]isoindolones) as potent dual CDK5/GSK3 inhibitors.
Universit£
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.
Palack£
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.
University Of Tours
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).
Icahn School Of Medicine At Mount Sinai
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.
Technische Universit£T Braunschweig
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.
Institut De Chimie Des Substances Naturelles
Synthesis and biological evaluation of tetrahydro[1,4]diazepino[1,2-a]indol-1-ones as cyclin-dependent kinase inhibitors.
Universit£
9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.
Technische Universit£T Braunschweig
Synthesis, biological evaluation and molecular modelling studies of 4-anilinoquinazoline derivatives as protein kinase inhibitors.
Rajiv Gandhi Proudyogiki Vishwavidyalaya
Synthesis of novel 7-substituted pyrido[2',3':4,5]furo[3,2-d]pyrimidin-4-amines and their N-aryl analogues and evaluation of their inhibitory activity against Ser/Thr kinases.
Cobra
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.
Universit£
6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity.
Universit£
Synthesis, resolution, and biological evaluation of atropisomeric (aR)- and (aS)-16-methyllamellarins N: unique effects of the axial chirality on the selectivity of protein kinases inhibition.
Nagasaki University
Synthesis, biological evaluation and molecular docking studies of pyrazole derivatives coupling with a thiourea moiety as novel CDKs inhibitors.
Nanjing University
Potential neuroprotective flavonoid-based inhibitors of CDK5/p25 from Rhus parviflora.
Kyung Hee University
A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.
Palack£
Structure-based optimization of oxadiazole-based GSK-3 inhibitors.
Technische Universit£T Darmstadt
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.
H. Lee Moffitt Cancer Center And Research Institute
Design, synthesis, and molecular modelling of pyridazinone and phthalazinone derivatives as protein kinases inhibitors.
University Of Strasburg
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.
Palack£
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.
University Of Athens
Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
Universitat De Barcelona
Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases.
Universit£
Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling.
University Of Paris
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.
TBA
Studying synergism of methyl linked cyclohexyl thiophenes with triazole: synthesis and their cdk5/p25 inhibition activity.
Dr. Reddy'S Laboratories, Ameerpet, Hyderabad, India.
Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease.
Pfizer
A novel approach to cyclin-dependent kinase 5/p25 inhibitors: A potential treatment for Alzheimer's disease.
Dr. Reddy'S Laboratories
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.
Cellzome
Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist.
TBA
Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
Universit£
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Cnrs
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.
Martin-Luther-University Halle-Wittenberg
A one-pot synthesis and biological activity of ageladine A and analogues.
Macquarie University
Synthesis and biological evaluation of N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors.
Universit£
Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Ka inhibitors.
Universit£
Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors.
Astrazeneca
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a.
Technische Universit£T Darmstadt
Synthesis and biological evaluation of analogs of the marine alkaloids granulatimide and isogranulatimide.
Universit£
Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases.
Institut De Chimie Des Substances Naturelles (Icsn)
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Amgen
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.
TBA
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.
Nerviano Medical Sciences Oncology
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
Nerviano Medical Sciences
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.
University Of California
TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone.
Cephalon
9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication.
Technische Universit£T Braunschweig
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.
University Of Oxford
Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease.
University Of Mississippi
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.
Vanderbilt University School Of Medicine
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.
Martin-Luther-University Halle-Wittenberg
Synthesis of chromeno[3,4-b]indoles as Lamellarin D analogues: a novel DYRK1A inhibitor class.
Universit£
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Synthesis and biological evaluation of new 3-(6-hydroxyindol-2-yl)-5-(Phenyl) pyridine or pyrazine V-Shaped molecules as kinase inhibitors and cytotoxic agents.
Universit£
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.
University Of South Florida
Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.
Technische Universit£T Darmstadt
Synthesis, protein kinase inhibitory potencies, and in vitro antiproliferative activities of meridianin derivatives.
Clermont Universite£
Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Universite£? De Rennes 1
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
Trinity College
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.
Nerviano Medical Sciences
Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity.
Palacky£? University And Institute Of Experimental Botany Ascr
Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors.
Harvard Medical School
Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25.
Duquesne University
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.
Martin-Luther-University Halle-Wittenberg
Identification of potent ITK inhibitors through focused compound library design including structural information.
Nycomed
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Amgen
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.
Nerviano Medical Sciences
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.
Universit£
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
Abbott Laboratories
Synthesis and antiproliferative activity of 7-azaindirubin-3'-oxime, a 7-aza isostere of the natural indirubin pharmacophore.
University Of Athens
Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors.
TBA
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.
Cgi Pharmaceuticals
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.
Takeda Pharmaceutical
Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors.
Laboratorio De Radicales Libres Y QuÍMica Computacional (Iqog, Csic)
Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins.
Clermont Universit£
Identification of potential cellular targets of aloisine A by affinity chromatography.
Cnrs Usr-3151
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.
University Of Illinois At Chicago
Synthesis and cytotoxic activity of new azepino[3',4':4,5]pyrrolo[2,1-a]isoquinolin-12-ones.
Universidad Nacional AutóNoma De MéXico
Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors.
Université
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.
Université
Clubbed thiazoles by MAOS: a novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer's disease.
Dr. Reddys Laboratories
A Pd(0) based cross-coupling approach to the synthesis of 2-amidopurines and their evaluation as CDK inhibitors.
Institut Curie
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9.
Banyu Tsukuba Research Institute
Synthesis and biological evaluation of novel phenylcarbazoles as potential anticancer agents.
Université
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.
Johnson & Johnson Pharmaceutical Research And Development
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.
Pfizer
A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors.
Pharmacia
Beta-carbolines as specific inhibitors of cyclin-dependent kinases.
Institute Of Molecular And Cell Biology
Chromone containing sulfonamides as potent carbonic anhydrase inhibitors.
Ondokuz Mayis University
Identification of Novel Selective Lysine-Specific Demethylase 1 (LSD1) Inhibitors Using a Pharmacophore-Based Virtual Screening Combined with Docking.
China Pharmaceutical University
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
Takeda Pharmaceutical
Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor.
Nerviano Medical Sciences
Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.
Universite De Lyon
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.
Astex
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.
Amgen
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.
Nerviano Medical Sciences
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.
Chinese Academy Of Sciences
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.
Cnrs
Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.
Institut Curie
Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors.
Institut Curie
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.
Technische Universitat Braunschweig
Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin.
Lawrence Berkeley National Laboratory
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.
Martin-Luther-University Halle-Wittenberg
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.
University Of Athens
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.
Faculte De Medecine Et De Pharmacie
Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.
Cnrs
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.
Universitat Hamburg