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 |
28049589 |
159 |
A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore. |
Sri International |
28039836 |
41 |
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities. |
East China Normal University |
28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
27448913 |
10 |
New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities. |
China Pharmaceutical University |
27171036 |
164 |
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
University of Nebraska Medical Center |
27297568 |
50 |
Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy. |
University of South Carolina |
26900761 |
4 |
Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS). |
Monash University (Parkville Campus) |
26881908 |
13 |
De Novo Design at the Edge of Chaos. |
Swiss Federal Institute of Technology (Eth) |
27173802 |
2 |
Sequential one-pot synthesis of bis(indolyl)glyoxylamides: Evaluation of antibacterial and anticancer activities. |
Birla Institute of Technology |
26951753 |
336 |
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
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 |
25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
24793884 |
151 |
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. |
Amgen |
24641103 |
104 |
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
Amgen |
12657252 |
15 |
Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors. |
Eli Lilly |
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 |
24286762 |
34 |
Fragment based discovery of arginine isosteres through REPLACE: towards non-ATP competitive CDK inhibitors. |
University of South Carolina |
23249297 |
75 |
Trimeric hemibastadin congener from the marine sponge Ianthella basta. |
Heinrich-Heine University |
24900658 |
10 |
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors. |
Hoffmann-La Roche |
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 |
10741557 |
26 |
Naphthyl ketones: a new class of Janus kinase 3 inhibitors. |
Astrazeneca |
16584130 |
95 |
Selectivity and potency of cyclin-dependent kinase inhibitors. |
Georgetown University |
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 |
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 |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
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 |
15267232 |
65 |
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
Eli Lilly |
10743948 |
22 |
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. |
Ewha Womans University |
10843211 |
38 |
Structure-activity relationship studies of flavopiridol analogues. |
Mitotix |
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 |
16476733 |
18 |
Inhibition of S/G2 phase CDK4 reduces mitotic fidelity. |
University of Queensland |
16249345 |
25 |
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. |
Glaxosmithkline |
22136433 |
67 |
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. |
Ludwig-Maximilians University of Munich |
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 |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
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 |
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 |
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 |
21035334 |
55 |
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors. |
Martin-Luther-University Halle-Wittenberg |
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 |
20925433 |
21 |
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
Aristotle University of Thessaloniki |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
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 |
20307980 |
22 |
B-Raf kinase inhibitors: hit enrichment through scaffold hopping. |
Wyeth Research |
19864136 |
45 |
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors. |
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 |
19632122 |
54 |
Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1. |
University of Leicester |
19362830 |
47 |
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors. |
Wyeth Research |
18835709 |
91 |
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors. |
Glaxosmithkline |
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 |
19211246 |
320 |
N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping. |
4Sc |
19053831 |
39 |
Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles. |
Institute of General Genetics |
18986805 |
39 |
Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. |
Astrazeneca Pharmaceuticals |
18815031 |
41 |
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors. |
Astrazeneca |
18650093 |
88 |
Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4. |
University of Leicester |
18529047 |
156 |
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. |
Eberhard-Karls University |
18494457 |
160 |
4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4). |
Wyeth Research |
16441060 |
12 |
A common protein fold topology shared by flavonoid biosynthetic enzymes and therapeutic targets. |
Griffith University |
10869191 |
15 |
Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases. |
Heinrich-Heine-UniversitäT |
18353638 |
71 |
Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors. |
Keimyung University |
17448574 |
3 |
1-Aryl-4,6-dihydropyrazolo[4,3-d][1]benzazepin-5(1H)-ones: a new class of antiproliferative agents with selectivity for human leukemia and breast cancer cell lines. |
Technische UniversitÄT Braunschweig |
17303421 |
56 |
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
Roche Research Center |
17188862 |
27 |
Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927. |
Wyeth Research |
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 |
16884302 |
209 |
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution. |
University of Auckland |
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 |
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 |
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 |
15546730 |
9 |
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
14552791 |
35 |
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
Eli Lilly |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
12036347 |
116 |
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes. |
Aventis Pharma Deutschland |
32184044 |
23 |
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs. |
Glaxosmithkline |
32305182 |
48 |
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
Shenyang Pharmaceutical University |
30639897 |
48 |
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures. |
The First Affiliated Hospital of Zhengzhou University |
32502343 |
79 |
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13. |
Harvard Medical School |
32150405 |
75 |
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? |
Lebanese American University |
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 |
31477350 |
80 |
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
Eli Lilly |
31382120 |
4 |
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
Nankai University |
31167153 |
8 |
An overview on the synthetic and medicinal perspectives of indenopyrazoles. |
Csir-Indian Institute of Chemical Technology |
31514062 |
80 |
Recent advances in the development of cyclin-dependent kinase 7 inhibitors. |
Tianjin University of Science and Technology |
31098000 |
63 |
Discovery of CDK5 Inhibitors through Structure-Guided Approach. |
University of South Australia |
31307887 |
64 |
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma. |
Genentech |
30943029 |
59 |
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. |
Palack£ |
31693351 |
473 |
Discovery of 4 |
TBA |
31376566 |
19 |
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer. |
Nankai University |
31381325 |
46 |
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents. |
Chengdu University |
30733087 |
53 |
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. |
China Pharmaceutical University |
30570265 |
9 |
Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis. |
University of Dundee |
30978559 |
38 |
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
University of Padova |
30927566 |
52 |
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
Shenyang Pharmaceutical University |
30543440 |
86 |
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. |
University of South Australia Cancer Research Institute |
30826188 |
25 |
Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. |
University of Science & Technology (Ust) |
30508668 |
62 |
Discovery of a highly selective FLT3 inhibitor with specific proliferation inhibition against AML cells harboring FLT3-ITD mutation. |
China Pharmaceutical University |
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 |
31846577 |
34 |
Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5- |
Northeastern University |
31670517 |
41 |
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms. |
West China Hospital of Sichuan University |
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 |
26505898 |
123 |
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. |
Novartis Institutes For Biomedical Research |
26560048 |
1 |
Discovery of a marine-derived bis-indole alkaloid fascaplysin, as a new class of potent P-glycoprotein inducer and establishment of its structure-activity relationship. |
Csir-Indian Institute of Integrative Medicine |
25835357 |
22 |
Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
Palack� |
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 |
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 |
23323521 |
52 |
Optimization of non-ATP competitive CDK/cyclin groove inhibitors through REPLACE-mediated fragment assembly. |
University of South Carolina |
19889545 |
34 |
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 |
19271717 |
96 |
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium. |
Heinrich-Heine-Universitat |
19091560 |
56 |
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: synthesis, biological evaluation, and structure-activity relationships. |
Daiichi Sankyo |
18494522 |
244 |
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense. |
Heinrich-Heine-Universit£T |
12762808 |
2 |
New sesquiterpene quinols from a Micronesian sponge, Aka sp. |
University of Oklahoma |
9599282 |
8 |
Spongiacidins A-D, new bromopyrrole alkaloids from hymeniacidon sponge |
Hokkaido University |
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 |
28911822 |
24 |
Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors. |
Central University of Punjab |
30197029 |
27 |
Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors. |
Jiangnan University |
29247857 |
102 |
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. |
Beijing Normal University |
29459274 |
69 |
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
Shanghai Haihe Pharmaceutical |
29429832 |
77 |
Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships. |
Beijing University of Technology |
29273417 |
26 |
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold. |
University of Kwazulu-Natal |
29074254 |
52 |
Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors. |
Shanghai Haihe Pharmaceutial |
29894944 |
66 |
Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
China Pharmaceutical University |
28494255 |
2 |
Design and synthesis of bis(indolyl)ketohydrazide-hydrazones: Identification of potent and selective novel tubulin inhibitors. |
Birla Institute of Technology |
29853338 |
31 |
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 |
29357250 |
80 |
Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. |
China Pharmaceutical University |
28651979 |
6 |
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate. |
Nankai University |
28259529 |
31 |
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
The Ohio State University |
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 |
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 |
28714692 |
232 |
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
University of Chinese Academy of Sciences |
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 |
34651447 |
87 |
A patent review on SARS coronavirus main protease (3CLpro) inhibitors. |
Experimental Drug Development Centre |
15950190 |
10 |
Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease. |
National Taiwan University |
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 |
24403173 |
12 |
Long residence times revealed by Aurora A kinase-targeting fluorescent probes derived from inhibitors MLN8237 and VX-689. |
University of Tartu |
16242653 |
33 |
A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. |
Gpc Biotech |
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 |
12244092 |
12 |
Structural basis for Chk1 inhibition by UCN-01. |
Glaxosmithkline |
16949284 |
34 |
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors. |
Johnson & Johnson Pharmaceutical |
16916797 |
8 |
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics. |
Incyte |
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 |
16942020 |
12 |
Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. |
University of Oxford |
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 |
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 |
15261277 |
30 |
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors. |
Cyclacel |
15027857 |
66 |
2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity. |
Cyclacel |
15081017 |
17 |
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors. |
Astrazeneca |
12941325 |
18 |
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation. |
Astrazeneca |
12941312 |
58 |
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines. |
Astrazeneca |
12941311 |
34 |
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines. |
Astrazeneca |
10969976 |
13 |
Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1. |
Korea Research Institute of Bioscience and Biotechnology |
11960485 |
18 |
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics. |
Novartis Pharmaceuticals |
15664865 |
37 |
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes. |
Martin-Luther-University Halle-Wittenberg |
15189033 |
48 |
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. |
Pharmacia Italia |
11311054 |
14 |
Indenopyrazoles as novel cyclin dependent kinase (CDK) inhibitors. |
Dupont Pharmaceuticals |
11354366 |
81 |
Quinazolines as cyclin dependent kinase inhibitors. |
Dupont Pharmaceuticals |
11514172 |
20 |
Identification of selective inhibitors of cyclin dependent kinase 4. |
Dupont Pharmaceuticals |
15482910 |
53 |
Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors. |
Dupont Pharmaceuticals |
12747775 |
56 |
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
Eli Lilly |
12824014 |
284 |
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
Eli Lilly |
14552792 |
53 |
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
Eli Lilly |
15149644 |
37 |
Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors. |
Eli Lilly |
15149678 |
32 |
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors. |
Eli Lilly |
15225699 |
27 |
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase 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 |
11741479 |
28 |
Structure-based generation of a new class of potent Cdk4 inhibitors: new de novo design strategy and library design. |
Banyu Tsukuba Research Institute |
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 |
14698155 |
68 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3. |
Bristol-Myers Squibb |
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 |
12431050 |
76 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern. |
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 |
12431051 |
114 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2). |
Bristol-Myers Squibb |