PMID

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Article Title

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Explicit treatment of active-site waters enhances quantum mechanical/implicit solvent scoring: Inhibition of CDK2 by new pyrazolo[1,5-a]pyrimidines.

Masaryk University

Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.

University of Nebraska Medical Center

RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.

Beni-Suef University

5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.

Palack£

Synthesis and pharmacological evaluation of dehydroabietic acid thiourea derivatives containing bisphosphonate moiety as an inducer of apoptosis.

Southeast University

Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents.

Egyptian Russian University

Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.

University of Tours

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

Identification of azabenzimidazoles as potent JAK1 selective inhibitors.

Astrazeneca

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

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 kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.

Siedlce University of Natural Sciences and Humanities

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

The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.

Amgen

Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode.

TBA

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

Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.

University of Queensland

5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.

Hanyang University

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 of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Ariad Pharmaceuticals

In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.

Astrazeneca R&D Boston

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Nerviano Medical Sciences

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

Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).

Nycomed Pharma

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

Cyclacel

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.

Institute of Science and Technology

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Nerviano Medical Sciences

Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.

East China University of Science & Technology

3,5,7-Substituted Pyrazolo[4,3-

Palack£

Discovery of 5,7-Dihydro-6

Incyte

Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.

Pfizer

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

Syros Pharmaceuticals

3

Purdue University

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

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

China Pharmaceutical University

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

Tetrahydroindazole inhibitors of CDK2/cyclin complexes.

University of Minnesota

First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.

Nankai 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

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

Potential of Cyclin-Dependent Kinase Inhibitors as Cancer Therapy.

Therachem Research Medilab

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

Astrazeneca

Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-

University of Edinburgh

Novel CDK2 Inhibitors for Treating Cancer.

Smith, Gambrell & Russell

Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.

The First Affiliated Hospital of Zhengzhou University

CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?

Lebanese American 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

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.

Genentech

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

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

Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances.

University of Science & Technology (Ust)

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

Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.

Eppley Institute For Research In Cancer and Allied Diseases

Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-

Takeda Pharmaceutical

Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).

Astrazeneca

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£

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

Synthesis, biological evaluation, and molecular docking studies of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives as novel anticancer agents.

Changzhou University

Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of cyclin D1-CDK4: synthesis, biological evaluation and structure-activity relationships. Part 2.

Daiichi Sankyo

1,3,5-Triazines: A promising scaffold for anticancer drugs development.

Universit£

ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles.

Palack£

A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.

Beijing Normal University

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

University of Kwazulu-Natal

Trisubstituted purine inhibitors of PDGFR? and their antileukemic activity in the human eosinophilic cell line EOL-1.

Palack£

Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.

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

2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase.

Takeda Pharmaceutical

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

A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.

Gpc Biotech

Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor.

Nerviano Medical Sciences

Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.

Amgen

Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.

Hoffmann-La Roche

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.

Nerviano Medical Sciences

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

Palacky University

Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.

Lawrence Berkeley National Laboratory

Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.

Chinese Academy of Sciences

Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.

Palacky University

3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.

Hoffmann-La Roche

A new series of potent oxindole inhibitors of CDK2.

Hoffmann-La Roche

Synthesis of potent oxindole CDK2 inhibitors.

Hoffmann-La Roche

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

Cyclacel

2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.

Cyclacel

Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.

Astrazeneca

Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors.

Astrazeneca

Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.

Astrazeneca

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.

Astrazeneca

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.

Astrazeneca

Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.

Martin-Luther-University Halle-Wittenberg

Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors.

Sugen

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.

Pharmacia Italia

Indenopyrazoles as novel cyclin dependent kinase (CDK) inhibitors.

Dupont Pharmaceuticals

Quinazolines as cyclin dependent kinase inhibitors.

Dupont Pharmaceuticals

Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors.

Dupont Pharmaceuticals

Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.

Eli Lilly

Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.

Eli Lilly

Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.

Eli Lilly

Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors.

Eli Lilly

1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors.

Eli Lilly

Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.

Eli Lilly

Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.

Avenida De La Industria

Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.

Eli Lilly

Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.

Pfizer

2-Aminoquinazoline inhibitors of cyclin-dependent kinases.

Naeja Pharmaceutical

Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.

Parke-Davis Pharmaceutical Research

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.

Bristol-Myers Squibb

Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.

Bristol-Myers Squibb

N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.

Bristol-Myers Squibb

1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.

Bristol-Myers Squibb

1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.

Bristol-Myers Squibb

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern.

Bristol-Myers Squibb

Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.

Bristol-Myers Squibb

Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).

Bristol-Myers Squibb