The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27391135 |
28 |
3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents. |
Egyptian Russian University |
| 27171036 |
164 |
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
University of Nebraska Medical Center |
| 27363938 |
2 |
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) |
| 27297568 |
50 |
Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy. |
University of South Carolina |
| 27055065 |
92 |
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. |
The Institute of Cancer Research |
| 27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang University |
| 27003761 |
120 |
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. |
Nerviano Medical Sciences |
| 27117263 |
51 |
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors. |
Takeda Pharmaceutical |
| 26762835 |
342 |
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 |
| 26222319 |
192 |
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. |
Nerviano Medical Sciences |
| 25007344 |
73 |
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics. |
Christian-Albrechts-University of Kiel |
| 24798019 |
30 |
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors. |
Institut De Chimie Des Substances Naturelles |
| 25010935 |
1 |
Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents. |
Jamia Hamdard (Hamdard University) |
| 23906342 |
14 |
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. |
Takeda Pharmaceutical |
| 24417566 |
43 |
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 |
| 24256217 |
177 |
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). |
The Institute of Cancer Research |
| 24286762 |
34 |
Fragment based discovery of arginine isosteres through REPLACE: towards non-ATP competitive CDK inhibitors. |
University of South Carolina |
| 23454515 |
66 |
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
Universit£ |
| 24185375 |
76 |
Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents. |
University of Nottingham |
| 17850214 |
99 |
The selectivity of protein kinase inhibitors: a further update. |
University of Dundee |
| 18232649 |
60 |
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 |
| 22148278 |
132 |
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase |
S Bio |
| 22036212 |
8 |
Synthesis of 6-(het) ary Xylocydine analogues and evaluating their inhibitory activities of CDK1 and CDK2 in vitro. |
Jilin University |
| 22000924 |
25 |
Design, synthesis and biological study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors. |
National Organization For Drug Control & Research |
| 21723120 |
100 |
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
Nerviano Medical Sciences |
| 20621478 |
37 |
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
Trinity College |
| 32435391 |
42 |
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and |
Angelini Pharma |
| 30639897 |
48 |
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures. |
The First Affiliated Hospital of Zhengzhou University |
| 32129996 |
166 |
Discovery and SARs of 5-Chloro- |
Anhui Medical University |
| 31846828 |
2 |
Development of selective mono or dual PROTAC degrader probe of CDK isoforms. |
Sichuan University and Collaborative Innovation Center of Biotherapy |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 30665142 |
41 |
Cink4T, a quinazolinone-based dual inhibitor of Cdk4 and tubulin polymerization, identified via ligand-based virtual screening, for efficient anticancer therapy. |
De Montfort University |
| 30755337 |
95 |
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952. |
Japan Tobacco |
| 31382120 |
4 |
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
Nankai University |
| 31098000 |
63 |
Discovery of CDK5 Inhibitors through Structure-Guided Approach. |
University of South Australia |
| 31272794 |
6 |
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
Chongqing Medical University |
| 30943029 |
59 |
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. |
Palack£ |
| 30733087 |
53 |
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. |
China Pharmaceutical University |
| 31238183 |
13 |
Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity. |
China Pharmaceutical University |
| 31254921 |
7 |
Discovery of novel pyrimidine-based benzothiazole derivatives as potent cyclin-dependent kinase 2 inhibitors with anticancer activity. |
Southern Medical University |
| 30565923 |
34 |
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology. |
Eberhard Karls University T£Bingen |
| 30978559 |
38 |
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
University of Padova |
| 30543440 |
86 |
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. |
University of South Australia Cancer Research Institute |
| 30384048 |
365 |
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 |
| 31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
| 30234987 |
232 |
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
Palack£ |
| 28156111 |
214 |
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 |
| 25368960 |
17 |
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 |
| 24304238 |
22 |
8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode. |
University of Oxford |
| 31200237 |
95 |
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 |
| 24015767 |
3 |
Drug discovery for neglected diseases: molecular target-based and phenotypic approaches. |
University of Dundee |
| 30165341 |
72 |
Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors. |
Jiangnan University |
| 30199702 |
24 |
A ?-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy. |
Universit£ |
| 29046238 |
17 |
1,3,5-Triazines: A promising scaffold for anticancer drugs development. |
Universit£ |
| 30197029 |
27 |
Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors. |
Jiangnan University |
| 29985601 |
64 |
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
Seoul National University |
| 30253346 |
46 |
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 |
| 30199249 |
92 |
Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N |
The Institute of Cancer Research |
| 30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
| 30026041 |
139 |
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition. |
University College Cork |
| 29550093 |
13 |
Discovery of novel CDK inhibitors via scaffold hopping from CAN508. |
Chinese Academy of Medical Sciences and Peking Union Medical College |
| 29273417 |
26 |
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold. |
University of Kwazulu-Natal |
| 29894944 |
66 |
Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
China Pharmaceutical University |
| 29778892 |
48 |
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors. |
University of Tours |
| 30091915 |
19 |
Development of Second-Generation CDK2 Inhibitors for the Prevention of Cisplatin-Induced Hearing Loss. |
TBA |
| 30067358 |
79 |
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 |
| 29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
| 29259738 |
74 |
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions. |
Vertex Pharmaceuticals |
| 29853332 |
50 |
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration. |
Universit£ |
| 29370702 |
41 |
Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor. |
Csir-Indian Institute of Integrative Medicine |
| 28827110 |
54 |
Synthesis and biological evaluation of N9-cis-cyclobutylpurine derivatives for use as cyclin-dependent kinase (CDK) inhibitors. |
Korea Research Institute of Chemical Technology |
| 27721154 |
660 |
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
University of Paris |
| 29144137 |
60 |
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 |
| 28487075 |
36 |
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 |
| 28557430 |
45 |
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 |
| | 113 |
CDK2-CyclinA in CSAR_FULL_RELEASE_3JULY2012 |
Csar |
| 16492568 |
12 |
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design. |
Cyclacel |
| 19827834 |
93 |
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control. |
Vertex Pharmaceuticals |
| 19200745 |
35 |
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta. |
Takeda Pharmaceutical |
| 19603809 |
59 |
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 |
| 19128055 |
24 |
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 |
| 19143567 |
49 |
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. |
Astex |
| 17098432 |
10 |
Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK). |
Paradigm Pharmaceuticals |
| 18656911 |
39 |
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design. |
Astex |
| 17570665 |
19 |
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping. |
Vernalis (R&D) |
| 12244092 |
12 |
Structural basis for Chk1 inhibition by UCN-01. |
Glaxosmithkline |
| 16289938 |
24 |
Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification. |
Vernalis (R&D) |
| 16616492 |
3 |
A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor. |
Nerviano Medical Sciences |
| 16290148 |
44 |
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors. |
Nerviano Medical Sciences |
| 17064068 |
36 |
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
Palacky University |
| 16325401 |
25 |
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. |
Vernalis (R&D) |
| 15686876 |
17 |
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2. |
Vernalis (R&D) |
| 15225695 |
64 |
4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors. |
Tsukuba Research Laboratories |
| 12941317 |
25 |
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis. |
Glaxosmithkline |
| 12941333 |
61 |
6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). |
Glaxosmithkline |
| 12699760 |
19 |
5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). |
Glaxosmithkline |
| 15341487 |
213 |
N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. |
Glaxosmithkline |
| 11728181 |
188 |
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis. |
Glaxosmithkline |
| 11960485 |
18 |
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics. |
Novartis Pharmaceuticals |
| 15713378 |
72 |
Benzodipyrazoles: a new class of potent CDK2 inhibitors. |
Nerviano Medical Sciences |
| 15189033 |
48 |
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. |
Pharmacia Italia |
| 15828833 |
29 |
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization. |
Nerviano Medical Sciences |
| 15974571 |
62 |
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. |
Johnson & Johnson Pharmaceutical |
| 11741480 |
41 |
A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues. |
Banyu Tsukuba Research Institute |
| 15801830 |
127 |
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4. |
Pfizer |
| 15993068 |
101 |
2-Aminoquinazoline inhibitors of cyclin-dependent kinases. |
Naeja Pharmaceutical |
| 15801831 |
94 |
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
Pfizer |
| 11101352 |
88 |
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
Parke-Davis Pharmaceutical Research |
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