PMID
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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
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
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 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, 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£
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
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.

Palack£
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
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
Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases.

Walter Reed Army Institute of Research
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
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University of Oxford
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.

The Institute of Cancer Research
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
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
Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.

Cyclacel
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.

Cyclacel
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 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
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
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
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
Advanced approaches of developing targeted covalent drugs.

College of Pharmacy
Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors.

Jinan University
Discovery, Optimization, and Evaluation of Selective CDK4/6 Inhibitors for the Treatment of Breast Cancer.

China Pharmaceutical University
Discovery and Optimization of Highly Selective Inhibitors of CDK5.

Goldfinc Bio
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 SY-5609: A Selective, Noncovalent Inhibitor of CDK7.

Syros Pharmaceuticals
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
Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold.

University of Campinas (Unicamp)
Discovery of

China Pharmaceutical University
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
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.

Sichuan University
Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.

University of Nottingham
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.

University of South Australia
Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors.

Cairo University
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.

China Pharmaceutical University
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
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.

Shanghaitech University
The Resurrection of Phenotypic Drug Discovery.

Temple 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
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)
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor.

Dana-Farber Cancer Institute
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.

Astrazeneca
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
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

Merck
Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ.

Korea Institute of Science and Technology
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
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.

Palack£
Discovery of 4

TBA
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.

China Pharmaceutical University
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
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.

Takeda Pharmaceutical
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
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.

Palack�
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
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
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.

University of Kwazulu-Natal
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
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 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
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.

Chinese Academy of Sciences
PREPARATION OF SUBSTITUTED 1,2-DIAMINOHETEROCYCLIC COMPOUND DERIVATIVES AND THEIR USE AS PHARMACEUTICAL AGENTS

Avelos Therapeutics
NOVEL QUINAZOLINONES THAT INHIBIT THE FORMATION OF TAU OLIGOMERS AND THEIR METHOD OF USE

Oligomerix
INHIBITORS OF MENIN-MLL INTERACTION

Biomea Fusion
SPIROCYCLIC-SUBSTITUTED 6,7-DIHYDRO-PYRANO[2,3-d]PYRIMIDINE INHIBITORS OF KRAS G12C MUTANT

Merck Sharp & Dohme
FUSED HETEROAROMATIC PYRROLIDINONES

Calithera Biosciences
PHENYL TRIAZOLE MLL1-WDR5 PROTEIN-PROTEIN INTERACTION INHIBITOR

Huyabio International
2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH

Bayer Aktiengesellschaft
Pyrazolo[3,4-B]pyridines and imidazo[1,5-B]pyridazines as PDE1 inhibitors

H. Lundbeck
2,6-diamino-3,4-dihydropyrimidin-4-one derivatives and use thereof in therapy

Thomas Helledays Stiftelse FÖR Medicinsk Forskning
Anti-inflammatory compound, and preparation and use thereof

E-Nitiate Biopharmaceuticals (Hangzhou)
Pyrazoloquinazolinone antitumor agents

Rockefeller University
Adrenergic receptor modulating compounds and methods of using the same

The Leland Stanford Junior University
Pyridylamino substituted heterotricyclic compounds, and preparation method and pharmaceutical use thereof

TBA
Therapeutic compounds and uses thereof

Genentech
Combination therapies using immuno-dash inhibitors and PGE2 antagonists

Tufts College
N4-hydroxycytidine and derivatives and anti-viral uses related thereto

Emory University
Pyrazolo[1,5-a]pyrazin-4-yl derivatives

Pfizer
Piperidine derivatives as inhibitors of ubiquitin specific protease 7

Almac Discovery
Heterocyclylamines as PI3K inhibitors

Incyte
Pyrrolopyridazine inhibitors of IRAK4 activity

Merck Sharp & Dohme
Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis.

University of Pavia
Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor.

University of Auckland
Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and oral bioavailability.

Sandoz Research Institute