The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
27643641 |
1 |
[1,2]Oxazolo[5,4-e]isoindoles as promising tubulin polymerization inhibitors. |
Universit£ |
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 |
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 |
26900761 |
4 |
Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS). |
Monash University (Parkville Campus) |
27189674 |
84 |
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 |
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£ |
26741853 |
95 |
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 |
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 |
26318056 |
25 |
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2. |
Universit£ |
26318067 |
34 |
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
Hanyang University |
26115571 |
38 |
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
Eli Lilly |
25262942 |
189 |
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping. |
Astrazeneca |
25768699 |
1 |
Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action. |
Universit£ |
24811300 |
20 |
Biased and unbiased strategies to identify biologically active small molecules. |
Institut De Chimie Des Substances Naturelles |
25589930 |
62 |
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. |
Lexicon Pharmaceuticals |
24798019 |
30 |
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors. |
Institut De Chimie Des Substances Naturelles |
24793884 |
151 |
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. |
Amgen |
24773549 |
20 |
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties. |
Development Center For Biotechnology |
24641103 |
104 |
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
Amgen |
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 |
24120542 |
90 |
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7. |
Amgen |
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 |
24157370 |
22 |
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors. |
Chugai Pharmaceutical |
24044867 |
86 |
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
Califia Bio |
23919303 |
3 |
Novel 1H-pyrrolo[2,3-b]pyridine derivative nortopsentin analogues: synthesis and antitumor activity in peritoneal mesothelioma experimental models. |
Universit£ |
23994326 |
9 |
6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity. |
Universit£ |
23933045 |
20 |
Synthesis, biological evaluation and molecular docking studies of pyrazole derivatives coupling with a thiourea moiety as novel CDKs inhibitors. |
Nanjing University |
23352510 |
37 |
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead. |
Roche Palo Alto |
23829517 |
30 |
A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors. |
Palack£ |
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 |
23399722 |
30 |
Synthesis and biological evaluation of guanidino analogues of roscovitine. |
Palack£ |
23354070 |
18 |
Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin. |
Universitat De Barcelona |
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 |
23218601 |
100 |
Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling. |
University of Paris |
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 |
24900493 |
12 |
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors. |
TBA |
22995819 |
4 |
Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine. |
TBA |
20627562 |
1 |
Cell cycle arrest and cytochrome c-mediated apoptotic induction by MCS-5A is associated with up-regulation of p16(INK4a) in HL-60 cells. |
Kyunggi-Do |
19879023 |
1 |
Synthesis and cytotoxic activity of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidine derivatives. |
Universidad Nacional Aut£Noma De M£Xico |
18232654 |
8 |
Pyrrolo[2,3-a]carbazoles as potential cyclin dependent kinase 1 (CDK1) Inhibitors. Synthesis, biological evaluation, and binding mode through docking simulations. |
University of Patras |
23082860 |
69 |
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
The Institute of Cancer Research |
22883026 |
34 |
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives. |
Takeda Pharmaceutical |
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 |
21381769 |
56 |
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
Universite£ |
24936234 |
42 |
Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist. |
TBA |
23083119 |
57 |
Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
Universit£ |
23063403 |
21 |
Recent results in protein kinase inhibition for tropical diseases. |
Montclair State University |
23039927 |
44 |
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases. |
Martin-Luther-University Halle-Wittenberg |
23021994 |
108 |
Identification of pyrimidine derivatives as hSMG-1 inhibitors. |
Pfizer |
22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
23085105 |
30 |
Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents. |
University of Nottingham |
22795331 |
51 |
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket. |
Janssen Pharmaceutical Companies of Johnson & Johnson |
24900482 |
32 |
Targeted kinase selectivity from kinase profiling data. |
TBA |
22372864 |
25 |
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases. |
Hanmi Research Center |
22607669 |
45 |
Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors. |
Biogen Idec |
24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
22326168 |
67 |
Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1. |
Biogen Idec |
24900361 |
27 |
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets. |
TBA |
21353571 |
26 |
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells. |
Hanyang University |
16584130 |
95 |
Selectivity and potency of cyclin-dependent kinase inhibitors. |
Georgetown University |
15559249 |
55 |
Pharmacological inhibitors of glycogen synthase kinase 3. |
The Rockefeller University |
18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
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 |
20097066 |
53 |
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme. |
Schering-Plough Research Institute |
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 |
19906467 |
109 |
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH). |
Technische Universit£T Braunschweig |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
19522465 |
102 |
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
Boehringer Ingelheim Pharma |
9677190 |
49 |
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. |
University of California |
18816110 |
27 |
Soluble 3',6-substituted indirubins with enhanced selectivity toward glycogen synthase kinase -3 alter circadian period. |
University of Athens |
18639462 |
22 |
Nitrogen-containing flavonoid analogues as CDK1/cyclin B inhibitors: synthesis, SAR analysis, and biological activity. |
Dalian University of Technology |
18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
17360485 |
10 |
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. |
Millennium Pharmaceuticals |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
18271520 |
423 |
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model. |
University of Zurich |
18191399 |
57 |
Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases. |
University of Auckland |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
17887663 |
34 |
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors. |
Pfizer |
16876403 |
85 |
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
16460940 |
13 |
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. |
Hoffmann-La Roche |
16451062 |
46 |
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. |
Astrazeneca |
15163202 |
16 |
Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis. |
Vanderbilt University School of Medicine |
12593668 |
6 |
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties. |
Martin-Luther-University Halle-Wittenberg |
12954055 |
47 |
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors. |
Johnson and Johnson Pharmaceutical Research and Development |
12930149 |
37 |
Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinases. |
Institute of Research |
12477352 |
85 |
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
Novartis Pharma |
11063606 |
137 |
3D-QSAR CoMFA on cyclin-dependent kinase inhibitors. |
Institut Curie |
12941319 |
15 |
2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors. |
Academy of Sciences of The Czech Republic |
12392733 |
13 |
Synthesis and biological activity of olomoucine II. |
Palack£ |
10843211 |
38 |
Structure-activity relationship studies of flavopiridol analogues. |
Mitotix |
9990463 |
69 |
2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors. |
Novartis Pharmaceuticals |
16476733 |
18 |
Inhibition of S/G2 phase CDK4 reduces mitotic fidelity. |
University of Queensland |
22269278 |
50 |
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation. |
Chugai Pharmaceutical |
15953730 |
13 |
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation. |
Hoffmann-La Roche |
22169262 |
26 |
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase. |
Shenyang Pharmaceutical University |
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 |
21982796 |
108 |
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors. |
The Institute of Cancer Research |
22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
21986585 |
2 |
A modular approach to trim cellular targets in anticancer drug discovery. |
Instituto Universitario De Bio-Org£Nica Antonio Gonz£Lez (Iubo-Ag) |
21936542 |
143 |
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
Novartis Institute For Biomedical Research |
21907583 |
48 |
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. |
University of South Florida |
21798738 |
44 |
Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I). |
Biogen Idec |
20810192 |
1 |
Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities--development of highly efficacious cytotoxic agents. |
Guru Nanak Dev University |
21684737 |
48 |
Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors. |
Keimyung University |
21627121 |
22 |
Irreversible Nek2 kinase inhibitors with cellular activity. |
University of California |
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 |
20630752 |
40 |
Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors. |
Millennium Pharmaceuticals |
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 |
21391610 |
139 |
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors. |
Vertex Pharmaceuticals |
21174434 |
13 |
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
Cylene Pharmaceuticals |
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 |
20684549 |
76 |
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor. |
Amgen |
20638755 |
15 |
Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay. |
University of Jordan |
20188579 |
42 |
Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase. |
Temple University |
18559524 |
21 |
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
Boehringer Ingelheim Austria |
20462263 |
127 |
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. |
Cyclacel |
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 |
20363627 |
56 |
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase. |
Universit£ |
20361800 |
22 |
5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. |
Institute of Science and Technology |
19894727 |
164 |
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent. |
Wyeth Research |
20346655 |
117 |
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases. |
Abbott Laboratories |
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 |
20188552 |
75 |
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). |
Wyeth Research |
19884006 |
47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
20167481 |
66 |
Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2. |
Sanofi-Aventis |
20166671 |
85 |
Selectively nonselective kinase inhibition: striking the right balance. |
Schering-Plough |
20137943 |
60 |
Azole-based inhibitors of AKT/PKB for the treatment of cancer. |
Amgen |
19994845 |
4 |
Synthesis and antiproliferative activity of 7-azaindirubin-3'-oxime, a 7-aza isostere of the natural indirubin pharmacophore. |
University of Athens |
19854649 |
49 |
Discovery of highly potent and selective type I B-Raf kinase inhibitors. |
Wyeth 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 |
20097074 |
5 |
New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme. |
Schering-Plough Research Institute |
20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
19945869 |
7 |
Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR. |
Taisho Pharmaceutical |
19945867 |
39 |
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR. |
Taisho Pharmaceutical |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19954867 |
2 |
Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors. |
Institute of Radiopharmacy |
19775160 |
79 |
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability. |
Takeda Pharmaceutical |
19616945 |
55 |
Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency. |
Pfizer |
19616942 |
45 |
Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency. |
Pfizer |
19203813 |
48 |
Synthesis and biological evaluation of 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as a novel class of potential anti-tumor agents. |
National Organization For Drug Control and Research |
18842409 |
28 |
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties. |
Sunesis Pharmaceuticals |
| 4 |
Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK II |
TBA |
| 42 |
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation |
TBA |
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 |
19317452 |
155 |
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4. |
Wyeth Research |
19286381 |
23 |
Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
18996007 |
30 |
The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing. |
Astrazeneca Pharmaceuticals |
18926699 |
30 |
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio. |
Sunesis Pharmaceuticals |
18718756 |
44 |
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity. |
Johnson & Johnson Pharmaceutical Research and Development |
18678484 |
57 |
A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity. |
Johnson & Johnson Pharmaceutical Research and Development |
18625560 |
3 |
Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors. |
Piramal Life Sciences |
18606543 |
68 |
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta. |
Wyeth Research |
18586356 |
40 |
Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors. |
Université |
18494457 |
160 |
4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4). |
Wyeth Research |
18393402 |
2 |
Natural products as leads to potential drugs: an old process or the new hope for drug discovery? |
National Cancer Institute-Frederick |
17981370 |
45 |
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies. |
Université |
17869387 |
158 |
Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases. |
University of Auckland |
17395594 |
10 |
Cellular characterization of a novel focal adhesion kinase inhibitor. |
University of Virginia |
11325241 |
2 |
Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species. |
Harbor Branch Oceanographic Institution |
18353638 |
71 |
Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors. |
Keimyung University |
17658776 |
109 |
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors. |
Abbott Laboratories |
17606372 |
66 |
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17532631 |
105 |
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents. |
Johnson & Johnson Pharmaceutical Research & Development |
17481894 |
64 |
4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation. |
Johnson & Johnson Pharmaceutical Research and Development |
17343372 |
143 |
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor. |
Abbott Laboratories |
17317182 |
36 |
Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1). |
Johnson & Johnson Pharmaceutical Research & Development |
17303421 |
56 |
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
Roche Research Center |
17287122 |
79 |
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. |
Abbott Laboratories |
17270437 |
68 |
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17178224 |
28 |
3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation. |
Keimyung University |
16870444 |
23 |
Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
16682186 |
16 |
Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. |
Johnson & Johnson Pharmaceutical Research & Development |
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 |
16644220 |
29 |
Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3. |
Université |
16460933 |
19 |
Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis. |
Cephalon |
16366598 |
51 |
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. |
Johnson & Johnson Pharmaceutical Research and Development |
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 |
15808450 |
52 |
Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors. |
Bayer Research Center |
15177482 |
90 |
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis. |
Novartis Institutes For Biomedical Research |
15149684 |
59 |
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
14640546 |
46 |
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin |
Cephalon |
14552791 |
35 |
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
Eli Lilly |
12941331 |
96 |
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
12941318 |
46 |
Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors. |
Academy of Sciences of The Czech Republic |
12941313 |
20 |
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. |
Novartis Pharma |
12039590 |
51 |
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck. |
Abbott Bioresearch Center |
12036377 |
3 |
Synthesis and antitumor activity of 1,5,6-substituted E-3-(2-chloro-3-indolylmethylene)-1,3-dihydroindol-2-ones. |
Università |
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 |
11597418 |
47 |
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity. |
Glaxosmithkline |
11378364 |
34 |
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. |
Research Biomet. Glaxo Wellcome Medicines Research Centre |
11012021 |
69 |
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. |
Basf Bioresearch |
10853665 |
104 |
Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src. |
Novartis Pharma |
10741555 |
9 |
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity. |
UniversitäT Hamburg |
10425100 |
43 |
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. |
UniversitäT Hamburg |
9871700 |
15 |
Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure. |
Kyushu University |
9046330 |
32 |
Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds. |
Charles University |
8691459 |
24 |
Alkyl and alkoxyethyl antineoplastic phospholipids. |
National Hellenic Research Foundation |
22957720 |
5 |
Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors. |
Ankara University |
24327656 |
9 |
The molecular chaperone Hsp70 activates protein phosphatase 5 (PP5) by binding the tetratricopeptide repeat (TPR) domain. |
University of Michigan |
25346381 |
6 |
Identification of Novel Selective Lysine-Specific Demethylase 1 (LSD1) Inhibitors Using a Pharmacophore-Based Virtual Screening Combined with Docking. |
China Pharmaceutical University |
23603658 |
33 |
Structure-guided design of a selective BCL-X(L) inhibitor. |
Walter and Eliza Hall Institute of Medical Research |
22296826 |
4 |
New active HIV-1 protease inhibitors derived from 3-hexanol: conformation study of the free inhibitors in crystalline state and in complex with the enzyme. |
Technical University of LÓDz |
16242653 |
33 |
A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. |
Gpc Biotech |
19572549 |
30 |
Identification of inhibitors of checkpoint kinase 1 through template screening. |
The Institute of Cancer Research |
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 |
19143567 |
49 |
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. |
Astex |
18307303 |
75 |
Discovery of selective aminothiazole aurora kinase inhibitors. |
Novartis |
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 |
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) |
15974586 |
29 |
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity. |
Vernalis (R&D) |
17064073 |
78 |
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 |
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 |
11170642 |
12 |
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717. |
Lawrence Berkeley National Laboratory |
16325401 |
25 |
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. |
Vernalis (R&D) |
15026054 |
55 |
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum. |
Cnrs |
12941317 |
25 |
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis. |
Glaxosmithkline |
15261277 |
30 |
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors. |
Cyclacel |
11881998 |
32 |
First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. |
Instituto De Quimica Medica (Csic) |
11728181 |
188 |
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis. |
Glaxosmithkline |
15189033 |
48 |
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. |
Pharmacia Italia |
15837297 |
33 |
3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation. |
Johnson & Johnson Pharmaceutical |
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 |
12747775 |
56 |
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
Eli Lilly |
15546737 |
59 |
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 |
15780638 |
45 |
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases. |
Eli Lilly |
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 |
15771433 |
30 |
Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. |
Johnson & Johnson Pharmaceutical |
16033269 |
98 |
Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors. |
Johnson & Johnson Pharmaceutical |
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 |
11101352 |
88 |
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
Parke-Davis Pharmaceutical Research |
15537345 |
171 |
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 |
12643928 |
24 |
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases. |
Bristol-Myers Squibb |
12824044 |
41 |
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. |
Bristol-Myers Squibb |
15125971 |
24 |
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases. |
Bristol-Myers Squibb |
11063609 |
36 |
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12190313 |
94 |
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
9357527 |
141 |
Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines. |
Novartis Pharmaceuticals |