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 |
26408454 |
51 |
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis. |
University Of South Australia |
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 |
26115571 |
38 |
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
Eli Lilly |
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 |
26071372 |
89 |
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3. |
Astellas Pharma |
25454794 |
1 |
Iterative conversion of cyclin binding groove peptides into druglike CDK inhibitors with antitumor activity. |
University Of South Carolina |
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 |
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 |
23249297 |
75 |
Trimeric hemibastadin congener from the marine sponge Ianthella basta. |
Heinrich-Heine University |
23312943 |
166 |
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
23312472 |
129 |
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
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 |
24900361 |
27 |
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets. |
TBA |
20932759 |
100 |
4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors. |
Nerviano Medical Sciences |
16584130 |
95 |
Selectivity and potency of cyclin-dependent kinase inhibitors. |
Georgetown University |
15559249 |
55 |
Pharmacological inhibitors of glycogen synthase kinase 3. |
The Rockefeller University |
20627564 |
51 |
Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases. |
Walter Reed Army Institute Of Research |
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 |
20038108 |
19 |
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance. |
Wyeth Research |
20030405 |
7 |
Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode. |
Peking University |
19854650 |
70 |
Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II. |
Amri |
19846305 |
86 |
Biaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part I. |
Amri |
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 |
15999997 |
85 |
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase. |
Serono Pharmaceutical Research Institute |
12852764 |
20 |
Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors. |
Novo Nordisk |
15013000 |
31 |
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. |
Glaxosmithkline |
22377675 |
44 |
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors. |
Westf£Lische Wilhelms-Universit£T M£Nster |
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 |
22154349 |
123 |
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 |
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 |
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 |
21907583 |
48 |
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. |
University Of South Florida |
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 |
21470862 |
110 |
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 |
21094608 |
74 |
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1. |
Merck Research Laboratories |
21094607 |
66 |
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2. |
Merck Research Laboratories |
21144757 |
15 |
Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25. |
Duquesne University |
20965724 |
57 |
Identification of potent ITK inhibitors through focused compound library design including structural information. |
Nycomed |
21038853 |
133 |
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6. |
Novartis Institutes For Biomedical Research |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
20817473 |
57 |
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. |
Nerviano Medical Sciences Oncology |
20483608 |
139 |
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck. |
Novartis Institute Of Biomedical Research |
20397705 |
208 |
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 |
20223663 |
100 |
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. |
Wyeth Research |
20045222 |
40 |
Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors. |
National Organization For Drug Control & Research |
19854645 |
87 |
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles. |
Wyeth Research |
20141146 |
234 |
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. |
Nerviano Medical Sciences |
18815031 |
41 |
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors. |
Astrazeneca |
17149885 |
20 |
Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor. |
Eberhard-Karls University |
17123821 |
21 |
Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues. |
University Of Kansas |
16750360 |
36 |
CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation. |
De Montfort University |
16384702 |
35 |
CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads. |
Genentech |
16216502 |
119 |
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors. |
Abbott Laboratories |
15999992 |
25 |
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 |
15566294 |
5 |
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. |
Università |
15149684 |
59 |
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
14505655 |
61 |
A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors. |
Pharmacia |
12182847 |
12 |
Peptide inhibitors of CDK2-cyclin A that target the cyclin recruitment-site: structural variants of the C-terminal Phe. |
University Of Nottingham |
12036347 |
116 |
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes. |
Aventis Pharma Deutschland |
11909733 |
30 |
Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
Institute Of Molecular And Cell Biology |
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 |