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166 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review

Article Title
Explicit treatment of active-site waters enhances quantum mechanical/implicit solvent scoring: Inhibition of CDK2 by new pyrazolo[1,5-a]pyrimidines.EBI
Masaryk University
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.EBI
University of Nebraska Medical Center
RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.EBI
Beni-Suef University
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.EBI
Synthesis and pharmacological evaluation of dehydroabietic acid thiourea derivatives containing bisphosphonate moiety as an inducer of apoptosis.EBI
Southeast University
Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents.EBI
Egyptian Russian University
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.EBI
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).EBI
Icahn School of Medicine At Mount Sinai
Identification of azabenzimidazoles as potent JAK1 selective inhibitors.EBI
Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.EBI
Chinese Academy of Medical Sciences and Peking Union Medical College
9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.EBI
Technische Universit£T Braunschweig
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.EBI
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.EBI
Siedlce University of Natural Sciences and Humanities
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).EBI
Icahn School of Medicine At Mount Sinai
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.EBI
Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode.EBI
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.EBI
Nerviano Medical Sciences
Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.EBI
University of Queensland
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.EBI
Nerviano Medical Sciences
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI
Hanyang University
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.EBI
Imperial College
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.EBI
Ariad Pharmaceuticals
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.EBI
Astrazeneca R&D Boston
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.EBI
Nerviano Medical Sciences
Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity.EBI
Palacky£? University and Institute of Experimental Botany Ascr
Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).EBI
Nycomed Pharma
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI
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.EBI
Nerviano Medical Sciences
5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.EBI
Institute of Science and Technology
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI
Nerviano Medical Sciences
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.EBI
East China University of Science & Technology
3,5,7-Substituted Pyrazolo[4,3-EBI
Discovery of 5,7-Dihydro-6EBI
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.EBI
Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7.EBI
Syros Pharmaceuticals
Purdue University
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.EBI
University of South Australia
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.EBI
China Pharmaceutical University
Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure.EBI
Institute For Organic Syntheses (Vuos)
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.EBI
Shanghaitech University
Tetrahydroindazole inhibitors of CDK2/cyclin complexes.EBI
University of Minnesota
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.EBI
Nankai University
The Resurrection of Phenotypic Drug Discovery.EBI
Temple University
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Beijing Normal University
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.EBI
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.EBI
China Pharmaceutical University
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.EBI
Egyptian Russian University
Potential of Cyclin-Dependent Kinase Inhibitors as Cancer Therapy.EBI
Therachem Research Medilab
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.EBI
Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-EBI
University of Edinburgh
Novel CDK2 Inhibitors for Treating Cancer.EBI
Smith, Gambrell & Russell
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.EBI
The First Affiliated Hospital of Zhengzhou University
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?EBI
Lebanese American University
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).EBI
Eli Lilly
Recent advances in the development of cyclin-dependent kinase 7 inhibitors.EBI
Tianjin University of Science and Technology
Discovery of CDK5 Inhibitors through Structure-Guided Approach.EBI
University of South Australia
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.EBI
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.EBI
Discovery of 4EBI
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.EBI
China Pharmaceutical University
Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity.EBI
China Pharmaceutical University
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.EBI
University of South Australia Cancer Research Institute
Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances.EBI
University of Science & Technology (Ust)
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI
University of Florida
Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.EBI
Eppley Institute For Research In Cancer and Allied Diseases
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-EBI
Takeda Pharmaceutical
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).EBI
3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights.EBI
Egyptian Russian University
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?EBI
Discovery of novel indirubin-3'-monoxime derivatives as potent inhibitors against CDK2 and CDK9.EBI
Chinese Academy of Medical Sciences and Peking Union Medical College
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.EBI
Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity.EBI
De Montfort University
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.EBI
Shanghai Pharmaceuticals Holding
Synthesis, biological evaluation, and molecular docking studies of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives as novel anticancer agents.EBI
Changzhou University
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of cyclin D1-CDK4: synthesis, biological evaluation and structure-activity relationships. Part 2.EBI
Daiichi Sankyo
1,3,5-Triazines: A promising scaffold for anticancer drugs development.EBI
ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles.EBI
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.EBI
Beijing Normal University
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.EBI
University of Kwazulu-Natal
Trisubstituted purine inhibitors of PDGFR? and their antileukemic activity in the human eosinophilic cell line EOL-1.EBI
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.EBI
Takeda Pharmaceutical
Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells.EBI
Shihezi University
2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase.EBI
Takeda Pharmaceutical
Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.EBI
University of Kaiserslautern
A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.BDB
Gpc Biotech
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.BDB
Nerviano Medical Sciences
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.BDB
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.BDB
Hoffmann-La Roche
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.BDB
Nerviano Medical Sciences
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.BDB
Palacky University
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.BDB
Lawrence Berkeley National Laboratory
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.BDB
Chinese Academy of Sciences
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.BDB
Palacky University
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.BDB
Hoffmann-La Roche
A new series of potent oxindole inhibitors of CDK2.BDB
Hoffmann-La Roche
Synthesis of potent oxindole CDK2 inhibitors.BDB
Hoffmann-La Roche
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.BDB
2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.BDB
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.BDB
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors.BDB
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.BDB
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.BDB
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.BDB
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.BDB
Martin-Luther-University Halle-Wittenberg
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors.BDB
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.BDB
Pharmacia Italia
Indenopyrazoles as novel cyclin dependent kinase (CDK) inhibitors.BDB
Dupont Pharmaceuticals
Quinazolines as cyclin dependent kinase inhibitors.BDB
Dupont Pharmaceuticals
Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors.BDB
Dupont Pharmaceuticals
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.BDB
Eli Lilly
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.BDB
Eli Lilly
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.BDB
Eli Lilly
Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors.BDB
Eli Lilly
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors.BDB
Eli Lilly
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.BDB
Eli Lilly
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.BDB
Avenida De La Industria
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.BDB
Eli Lilly
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.BDB
2-Aminoquinazoline inhibitors of cyclin-dependent kinases.BDB
Naeja Pharmaceutical
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.BDB
Parke-Davis Pharmaceutical Research
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.BDB
Bristol-Myers Squibb
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.BDB
Bristol-Myers Squibb
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.BDB
Bristol-Myers Squibb
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.BDB
Bristol-Myers Squibb
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.BDB
Bristol-Myers Squibb
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern.BDB
Bristol-Myers Squibb
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.BDB
Bristol-Myers Squibb
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.BDB
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.BDB
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).BDB
Bristol-Myers Squibb