The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28249207 |
78 |
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis. |
East China Normal University |
28692292 |
73 |
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers. |
Sichuan University And Collaborative Innovation Center For Biotherapy |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
28005359 |
66 |
Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines. |
Newcastle University |
27940419 |
31 |
Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands. |
Comenius University In Bratislava |
28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University Of Sydney |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
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) |
27078757 |
121 |
Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R). |
Astrazeneca |
26985305 |
34 |
Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells. |
Genentech |
26851505 |
65 |
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£ |
25914804 |
20 |
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 |
26408454 |
51 |
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis. |
University Of South Australia |
26349627 |
133 |
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9. |
The University Of Melbourne |
25262942 |
189 |
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping. |
Astrazeneca |
25730262 |
195 |
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A. |
Technische Universit£T Braunschweig |
24798019 |
30 |
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors. |
Institut De Chimie Des Substances Naturelles |
24973661 |
10 |
9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma. |
Technische Universit£T Braunschweig |
24793884 |
151 |
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. |
Amgen |
24742150 |
101 |
Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors. |
Vichem Chemie |
24120542 |
90 |
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7. |
Amgen |
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 |
23994326 |
9 |
6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity. |
Universit£ |
23937569 |
22 |
Selectivity data: assessment, predictions, concordance, and implications. |
Eli Lilly |
23867602 |
122 |
Lead identification of novel and selective TYK2 inhibitors. |
Genentech |
23829517 |
30 |
A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors. |
Palack£ |
23726345 |
41 |
Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus. |
Boehringer Ingelheim (Canada) |
23600925 |
12 |
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases. |
H. Lee Moffitt Cancer Center And Research Institute |
23301767 |
154 |
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 |
22770608 |
35 |
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
Palack£ |
23252711 |
46 |
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 |
20146435 |
60 |
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 |
22982525 |
32 |
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors. |
TBA |
22726925 |
216 |
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease. |
Cellzome |
22998443 |
69 |
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
Cnrs |
23085105 |
30 |
Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents. |
University Of Nottingham |
22339472 |
148 |
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth |
S Bio |
22465635 |
95 |
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. |
Abbott Laboratories |
18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
20138512 |
82 |
Discovery of potent and bioavailable GSK-3beta inhibitors. |
Roche Palo Alto |
20153204 |
109 |
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 |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University Of Oxford |
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 |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
22225635 |
5 |
Synthesis and biological evaluation of benzo[d]imidazole derivatives as potential anti-cancer agents. |
University Of Nottingham |
22014550 |
337 |
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
Ansaris |
21982796 |
108 |
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors. |
The Institute Of Cancer Research |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
21907583 |
48 |
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. |
University Of South Florida |
21777997 |
1 |
The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
Palack£ |
21080703 |
20 |
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 |
20621478 |
37 |
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
Trinity College |
21417417 |
8 |
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 |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
20462263 |
127 |
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. |
Cyclacel |
18842409 |
28 |
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties. |
Sunesis Pharmaceuticals |
19555113 |
45 |
Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships. |
Nerviano Medical Sciences |
19338355 |
104 |
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
University Of Illinois At Chicago |
18926699 |
30 |
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio. |
Sunesis Pharmaceuticals |
16682184 |
25 |
Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9. |
Banyu Tsukuba Research Institute |
29518312 |
78 |
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 |
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 |
9650799 |
159 |
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
Novartis Pharma |
19115845 |
39 |
First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. |
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 |
19007108 |
32 |
Synthetic and Crystallographic Studies of a New Inhibitor Series Targeting Bacillus anthracis Dihydrofolate Reductase. |
University Of Connecticut |
17228885 |
10 |
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation. |
Universita Di Pisa |
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 |
15261277 |
30 |
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors. |
Cyclacel |