PMID

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Article Title

Organization

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.

Universit£

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 PI3K? inhibitors.

Merck

Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase I? and ?.

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.

Universit£

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

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

3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.

Merck Research Laboratories

4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.

Palacky University

Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.

Cyclacel