157 articles for thisTarget
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Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect isletβ-cells from apoptosis.
East China Normal University
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.
Sichuan University and Collaborative Innovation Center For Biotherapy
A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.
Sri International
New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities.
China Pharmaceutical University
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
University of Nebraska Medical Center
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
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.
Merck Research Laboratories
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).
Icahn School of Medicine At Mount Sinai
Synthesis, biological evaluation and molecular docking studies of pyrazole derivatives coupling with a thiourea moiety as novel CDKs inhibitors.
Nanjing University
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.
H. Lee Moffitt Cancer Center and Research Institute
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
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Pfizer
p16(INK4a) Peptide mimetics identified via virtual screening.
Veterans Affairs Medical Center
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
TBA
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
Recent results in protein kinase inhibition for tropical diseases.
Montclair State University
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
Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases.
Walter Reed Army Institute of Research
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
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
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.
Martin-Luther-University Halle-Wittenberg
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.
Novartis Institutes For Biomedical Research
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University of Thessaloniki
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
A common protein fold topology shared by flavonoid biosynthetic enzymes and therapeutic targets.
Griffith University
Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor.
Henan University of Chinese Medicine
Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents:
Misr International University
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery.
Sichuan University
Palbociclib and Michael-acceptor hybrid compounds as CDK4/6 covalent inhibitors: Improved potency, broad anticancer spectrum and overcoming drug resistance.
Southeast University
A comprehensive insight on the recent development of Cyclic Dependent Kinase inhibitors as anticancer agents.
Mizoram University
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.
Sichuan University
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.
East China University of Science & Technology
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Menoufia University
Discovery of a Novel Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2) and Cyclin-Dependent Kinase 4 (CDK4) Dual Inhibitor for the Treatment of Triple-Negative Breast Cancer.
China Pharmaceutical University
Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9.
Banyu Tsukuba Research Institute
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.
China Pharmaceutical University
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
Zhengzhou University
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.
Hefei University of Technology
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
Csir-Indian Institute of Integrative Medicine
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
Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer.
Shandong First Medical University & Shandong Academy of Medical Sciences
Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold.
Stanford University
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.
Rapt Therapeutics
Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy.
Anhui Medical University
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
Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT.
Zhejiang 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
Indirubin Derivatives as Dual Inhibitors Targeting Cyclin-Dependent Kinase and Histone Deacetylase for Treating Cancer.
Guizhou Medical University
Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.
Chinese Academy of Sciences
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
Chinese Academy of Sciences
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.
Sichuan University
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.
China Pharmaceutical University
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.
Shanghaitech University
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.
Nankai University
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.
China Pharmaceutical University
Anticancer potential of some imidazole and fused imidazole derivatives: exploring the mechanism
Central University of Punjab
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
China Pharmaceutical University
Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
Key Laboratory of Biomedical Materials of Natural Macromolecules (Beijing University of Chemical Technology)
Potential of Cyclin-Dependent Kinase Inhibitors as Cancer Therapy.
Therachem Research Medilab
Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells.
Peking Union Medical College
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Astrazeneca
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs.
Glaxosmithkline
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
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?
Lebanese American University
Cink4T, a quinazolinone-based dual inhibitor of Cdk4 and tubulin polymerization, identified via ligand-based virtual screening, for efficient anticancer therapy.
De Montfort University
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).
Eli Lilly
Recent advances in the development of cyclin-dependent kinase 7 inhibitors.
Tianjin University of Science and Technology
Discovery of CDK5 Inhibitors through Structure-Guided Approach.
University of South Australia
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
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.
University of Padova
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.
University of South Australia Cancer Research Institute
Discovery of a highly selective FLT3 inhibitor with specific proliferation inhibition against AML cells harboring FLT3-ITD mutation.
China Pharmaceutical University
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
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.
West China Hospital of Sichuan University
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 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
Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors.
Jiangnan University
Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.
Central University of Punjab
Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors.
Jiangnan University
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.
Beijing Normal University
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.
Shanghai Haihe Pharmaceutical
Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships.
Beijing University of Technology
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.
University of Kwazulu-Natal
Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors.
Shanghai Haihe Pharmaceutial
Discovery of the selective and efficacious inhibitors of FLT3 mutations.
China Pharmaceutical University
Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells.
Shihezi University
Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.
China Pharmaceutical 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
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.
University of Chinese Academy of Sciences
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.
University of Kaiserslautern
IMIDAZOTRIAZINE THIOBENZAMIDE DERIVATIVE, AND PREPARATION METHOD AND APPLICATION THEREOF
Yunbaiyao Zhengwu Science and Technology (Shanghai) Co.
NOVEL QUINAZOLINONES THAT INHIBIT THE FORMATION OF TAU OLIGOMERS AND THEIR METHOD OF USE
Oligomerix
ARYLAMIDE COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Sichuan Kelun-Biotech Biopharmaceutical
MULTI-CYCLIC IRAK AND FLT3 INHIBITING COMPOUNDS AND USES THEREOF
Children'S Hospital Medical Center
CDK6/DYRK2 DUAL-TARGET INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Jiangsu Tasly Diyi Pharmaceutical
2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH
Bayer Aktiengesellschaft
5-membered and bicyclic heterocyclic amides as inhibitors of ROCK
Bristol-Myers Squibb
Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
Incyte
Substituted pyridine derivatives useful as C-FMS kinase inhibitors
Janssen Pharmaceutica
Substituted bridged diazepane derivatives and use thereof as TASK-1 and TASK-3 inhibitors
Bayer Pharma Aktiengesellschaft
Combination therapies using immuno-dash inhibitors and PGE2 antagonists
Tufts College
Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders
Achillion Pharmaceuticals
Substituted pyrimidines as cyclin-dependent kinase inhibitors
Shanghai Pharmaceuticals Holding
Tricyclic fused derivatives of 1-(cyclo)alkyl pyridin-2-one useful for the treatment of cancer
Jubilant Biosys
Substituted pyrimidines as cyclin-dependent kinase inhibitors
Shanghai Pharmaceuticals Holding
Substituted pyrrolopyrimidine CDK inhibitor, pharmaceutical composition containing same and use thereof
Chia Tai Tianqing Pharmaceutical Group
2,4-disubstituted pyrimidines as CDK inhibitors
Shanghai Xunhe Pharmaceutical Technology
Potent and selective inhibitors of monoamine transporters; method of making; and use thereof
The United States of America, As Represented By The Secretary, Department of Health and Human Services Office of Technology Transfer, National Institutes of Health
The preparation, in vitro screening and molecular docking of symmetrical bisquaternary cholinesterase inhibitors containing a but-(2E)-en-1,4-diyl connecting linkage.
University of Defence
17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivative, use thereof, and medicament containing the derivative
TBA
Substituted pyrido[2,3-d]pyrimidin-7(8H)-ones and therapeutic uses thereof
Temple University
In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine.
National Cancer Institute-Bethesda