PMID

Data

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

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

The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.

Amgen

Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.

Universit£

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£

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

Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.

Chinese Academy Of Sciences

3

Purdue University

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

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.

Universit£

Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1.

Universit£

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

The Resurrection of Phenotypic Drug Discovery.

Temple University School Of Pharmacy

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

Cyclin-Dependent Kinase Inhibitors in Cancer Therapeutics.

Usona 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

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

Discovery and SARs of 5-Chloro-

Anhui Medical University

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£

Discovery of BAY-985, a Highly Selective TBK1/IKK? Inhibitor.

Bayer

Discovery of 4

TBA

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

Novel arylazopyrazole inhibitors of cyclin-dependent kinases.

Palack�

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.

Universit£

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

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.

Universit£

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

First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.

Nerviano Medical 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

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