140 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.
Newcastle University
Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.
Comenius University In Bratislava
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
University of Nebraska Medical Center
A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.
India Academy of Scientific & Innovative Research (Acsir)
Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.
Genentech
Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.
Chinese Academy of Medical Sciences and Peking Union Medical College
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis.
University of South Australia
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.
The University of Melbourne
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.
Institut De Chimie Des Substances Naturelles
9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.
Technische Universit£T Braunschweig
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.
Amgen
Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors.
Vichem Chemie
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.
University of Rennes 1
Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.
University of Nottingham
6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity.
University of Turin
A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.
Palack£
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.
University of Nottingham
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.
Palack£
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.
University of Oxford
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors.
University of St. Andrews
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.
TBA
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Cnrs
Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents.
University of Nottingham
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
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
Synthesis and biological evaluation of benzo[d]imidazole derivatives as potential anti-cancer agents.
University of Nottingham
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.
The Institute of Cancer Research
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.
University of South Florida
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.
Imperial College
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
Trinity College
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
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.
Cyclacel
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.
Astrazeneca
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.
East China University of Science & Technology
Discovery of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and selective CDK9 inhibitors that enable transient target engagement for the treatment of hematologic malignancies.
China Pharmaceutical University
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.
The People'S Hospital of Xinjiang Uyghur Autonomous Region
Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold.
Stanford University
Current progress and novel strategies that target CDK12 for drug discovery.
West China Hospital
Discovery, Optimization, and Evaluation of Selective CDK4/6 Inhibitors for the Treatment of Breast Cancer.
China Pharmaceutical University
Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma.
China Pharmaceutical University
Discovery of Dual CDK6/PIM1 Inhibitors with a Novel Structure, High Potency, and Favorable Druggability for the Treatment of Acute Myeloid Leukemia.
China Pharmaceutical University
Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.
Chinese Academy of Sciences
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.
Harvard Medical School
Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.
University of Nottingham
Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion.
China Pharmaceutical University
In vitro identification of imidazo[1,2-a]pyrazine-based antileishmanial agents and evaluation of L. major casein kinase 1 inhibition.
University of Nantes
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1.
Paris-Saclay University
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.
China Pharmaceutical University
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.
University Paris-Saclay
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.
Shanghai Pharmaceuticals Holding
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.
Sichuan University/Collaborative Innovation Center of Biotherapy
Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure.
Institute For Organic Syntheses (Vuos)
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.
Shanghaitech University
Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
University of South Australia
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Endotherm
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.
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.
Egyptian Russian University
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Astrazeneca
Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors.
North-West University
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.
The First Affiliated Hospital of Zhengzhou University
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.
Harvard Medical School
Development of selective mono or dual PROTAC degrader probe of CDK isoforms.
Sichuan University and Collaborative Innovation Center of Biotherapy
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.
Merck
Cink4T, a quinazolinone-based dual inhibitor of Cdk4 and tubulin polymerization, identified via ligand-based virtual screening, for efficient anticancer therapy.
De Montfort University
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).
Eli Lilly
Discovery of CDK5 Inhibitors through Structure-Guided Approach.
University of South Australia
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.
Palack£
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.
Nankai University
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.
China Pharmaceutical University
Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity.
China Pharmaceutical University
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.
University of South Australia Cancer Research Institute
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.
University of Florida
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights.
Egyptian Russian University
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?
Palack£
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation.
University of South Australia
Discovery of novel indirubin-3'-monoxime derivatives as potent inhibitors against CDK2 and CDK9.
Chinese Academy of Medical Sciences and Peking Union Medical College
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.
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.
Shanghai Pharmaceuticals Holding
A ?-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.
University of Poitiers
1,3,5-Triazines: A promising scaffold for anticancer drugs development.
University of Palermo
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Astrazeneca
Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.
Chinese Academy of Sciences
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.
University College Cork
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.
Shanghai Haihe Pharmaceutical
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.
Chinese Academy of Medical Sciences and Peking Union Medical College
Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma.
Semmelweis University
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.
University of Kwazulu-Natal
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.
University of Tours
Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.
Takeda Pharmaceutical
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.
University of Nantes
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.
Nankai University
Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.
Csir-Indian Institute of Integrative Medicine
Synthesis and biological evaluation of N9-cis-cyclobutylpurine derivatives for use as cyclin-dependent kinase (CDK) inhibitors.
Korea Research Institute of Chemical Technology
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.
University of Paris
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.
Csir-Indian Institute of Integrative Medicine
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.
Nankai University
N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1?/? inhibitors: Synthesis, biological evaluation and molecular modeling studies.
Rajiv Gandhi Proudyogiki Vishwavidyalaya
PHENYL TRIAZOLE MLL1-WDR5 PROTEIN-PROTEIN INTERACTION INHIBITOR
Huyabio International
Combination therapies using immuno-dash inhibitors and PGE2 antagonists
Trustees of Tufts College
Piperidine derivatives as inhibitors of ubiquitin specific protease 7
Almac Discovery
Analysis of saponins and phenolic compounds as inhibitors of a-carbonic anhydrase isoenzymes.
Ege University
Slowly on, Slowly off: Bisubstrate-Analogue Conjugates of 5-Iodotubercidin and Histone H3 Peptide Targeting Protein Kinase Haspin.
University of Tartu
Triazinoindole analogs as potent inhibitors of a-glucosidase: synthesis, biological evaluation and molecular docking studies.
Hazara University
Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis.
University of Pavia