231 articles for thisTarget
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Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.
Ku Leuven
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.
Chinese Academy Of Sciences
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
Duquesne University
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.
Shenyang Pharmaceutical University
Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor.
National Taiwan University
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.
Chinese Academy Of Sciences
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.
Shenyang Pharmaceutical University
Discovery andw biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors.
Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Zhejiang University
Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
Southeast University
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
Duquesne University
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents.
Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.
Qilu Pharmaceutical
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.
Chinese Academy Of Sciences
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
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.
Chinese Academy Of Sciences
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Nerviano Medical Sciences
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.
Chinese Academy Of Sciences
Design, synthesis, and structure-activity relationships of novel 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.
Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors.
Nanjing University Of Technology
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
Quinazoline-based multi-tyrosine kinase inhibitors: synthesis, modeling, antitumor and antiangiogenic properties.
University Of Padova
Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs).
East China University Of Science And Technology
Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.
Takeda Pharmaceutical
Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.
Pfizer
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.
Takeda Pharmaceutical
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.
Takeda Pharmaceutical
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.
East China University Of Science And Technology
Synthesis and biological activity of 5-chloro-N4-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.
Duquesne University
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatic and antitumor agents.
Duquesne University
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.
Sichuan University
Trimeric hemibastadin congener from the marine sponge Ianthella basta.
Heinrich-Heine University
Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp.
Institute Of Microbial Chemistry (Bikaken)
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
National Center For Advancing Translational Sciences
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Exelixis
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Exelixis
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.
Takeda Pharmaceutical
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
Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.
TBA
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
University Of Genoa
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.
National Institute Of Biological Sciences
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.
Exelixis
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.
Takeda Pharmaceutical
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
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.
Duquesne University
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.
Sichuan University
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.
Takeda Pharmaceutical
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
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Ambit Biosciences
Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.
Astrazeneca
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Abbott Laboratories
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
TBA
Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.
Duquesne University
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.
Chinese Academy Of Sciences
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.
National Taiwan University
Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.
Duquesne University
Discovery and development of aurora kinase inhibitors as anticancer agents.
Vertex Pharmaceuticals
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Bristol-Myers Squibb
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Amgen
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University Of Oxford
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.
Osi Pharmaceuticals
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.
Targegen
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
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.
Novartis Pharma
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.
Millennium Pharmaceuticals
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.
Westf£Lische Wilhelms-Universit£T M£Nster
N¿?¿-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.
Duquesne University
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.
University Of Kentucky
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.
Glaxosmithkline
Effects of the indolocarbazole 3744W on the tyrosine kinase activity of the cytoplasmic domain of the platelet-derived growth factor beta-receptor.
Wellcome Research Laboratories
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
Millennium Pharmaceuticals
Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.
Astrazeneca
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.
Shenyang Pharmaceutical University
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
Shionogi
N¿?¿-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.
Duquesne University
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.
Takeda Pharmaceutical
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
Pfizer
Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.
Chinese Academy Of Sciences
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.
East China University Of Science And Technology
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
TBA
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.
National University Of Ireland
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
University Of Regensburg
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.
Martin-Luther-University Halle-Wittenberg
Identification of potent ITK inhibitors through focused compound library design including structural information.
Nycomed
Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
Shanghai Hengrui Pharmaceuticals
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University Of Thessaloniki
Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors.
Astrazeneca
Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.
Industrial Technology Research Institute
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.
Takeda Pharmaceutical
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.
Novartis Institutes For Biomedical Research
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.
Boehringer Ingelheim Austria
Rational design of inhibitors that bind to inactive kinase conformations.
Novartis Research Foundation
Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish.
Dana-Farber Cancer Institute
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile.
Development Center For Biotechnology
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.
Duquesne University
The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines.
Duquesne University
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.
Cgi Pharmaceuticals
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.
Ambit Biosciences
Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.
Hadassah Hebrew University Hospital
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.
The Institute Of Cancer Research
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Ambit Biosciences
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
Hanmi Research Center
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
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation
TBA
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
University Of Regensburg
N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.
4Sc
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
Novartis Institutes For Biomedical Research
5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.
Mahidol University
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.
Astrazeneca R&D Boston
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
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Glaxosmithkline
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
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
Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.
Duquesne University
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Genomics Institute Of The Novartis Research Foundation
Entry into a new class of protein kinase inhibitors by pseudo ring design.
Novartis Institutes For Biomedical Research
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.
Glaxosmithkline
4-Amino-6-piperazin-1-yl-pyrimidine-5-carbaldehyde oximes as potent FLT-3 inhibitors.
Johnson And Johnson Pharmaceutical Research And Development
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
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
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
Targegen
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
University Of Regensburg
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Pharmaceutical Research Institute
(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
Naphthofuroquinone derivatives: inhibition of receptor tyrosine kinases.
Korea Research Institute Of Chemical Technology
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor.
In Vivo Sciences Millennium Pharmaceuticals
Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.
Sugen
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
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
Pharmaceutical Research Institute
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.
Aventis Pharmaceuticals
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
Kyowa Hakko Kogyo
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.
Pharmaceutical Research Institute
Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases.
Sugen
Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.
King Fahd University Of Petroleum & Minerals
Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors.
Shandong University
Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.
Glaxosmithkline
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.
Aimst University
Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor.
Neurocrine Biosciences
Identification and characterization of a novel RF-amide peptide ligand for orphan G-protein-coupled receptor SP9155.
Schering-Plough Research Institute
S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine.
Centre De Recherches De Croissy
Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist.
UniversitÉ
Evaluation of the activities of pyrimethamine analogs against Plasmodium vivax and Plasmodium falciparum dihydrofolate reductase-thymidylate synthase using in vitro enzyme inhibition and bacterial complementation assays.
National Center For Genetic Engineering And Biotechnology At Thailand
Influence of side-chain structure of aliphatic amino acids on binding to isoleucyl-tRNA synthetase from Escherichia coli MRE 600.
Gesellschaft Fur Molekularbiolische Forschung Mbh
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Abbott Laboratories
Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.
Abbott Laboratories
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
Abbott Laboratories
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.
Gsk
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.
Genentech
Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.
Berlex
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.
Vernalis (R&D)
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.
Pfizer
Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX.
Canadian Institutes Of Health Research
Development of dihydropyridone indazole amides as selective rho-kinase inhibitors.
Glaxosmithkline
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.
Abbott Laboratories
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.
Abbott Laboratories
Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S.
Georgia State University
Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir.
Johnson & Johnson Pharmaceutical
Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase.
Merck Frosst Center For Therapeutic Research
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.
Incyte
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase i
Bristol-Myers Squibb
Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.
University Of Michigan
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Bristol-Myers Squibb
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
Bristol-Myers Squibb Pharmaceutical Research Institute
Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
Bristol-Myers Squibb
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Abbott Laboratories
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
Abbott Laboratories
Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.
Glaxosmithkline
Novel potent hepatitis C virus NS3 serine protease inhibitors derived from proline-based macrocycles.
Schering-Plough Research Institute
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.
University Of Antwerp
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.
Universita Degli Studi Di Firenze
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.
Merck Research Laboratories
Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.
University Of Oxford
Structural Insight into the Stereoselective Inhibition of MMP-8 by Enantiomeric Sulfonamide Phosphonates.
Istituto Di Cristallografia
Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide.
Pfizer
Structure-based design of nonpeptide inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1).
Pfizer
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.
Universidad Central De Venezuela
Inhibitors of the Diadenosine Tetraphosphate Phosphorylase Rv2613c of Mycobacterium tuberculosis.
University Of Konstanz
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Palacky University
Fluoroaromatic-fluoroaromatic interactions between inhibitors bound in the crystal lattice of human carbonic anhydrase II.
University Of Pennsylvania
Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease.
Hawaii Biotech
Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.
Istituto Di Biostrutture E Bioimmagini-Cnr
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.
University Of Agricultural Sciences And Veterinary Medicine
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.
Hoffmann-La Roche
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors.
Santhera Pharmaceuticals
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.
Lawrence Berkeley National Laboratory
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.
Vernalis (R&D)
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.
Vernalis (R&D)
Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors.
Qingdao University
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
University Of Bologna
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.
University Of North Carolina At Chapel Hill
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.
Merck Frosst Canada
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.
Merck Research Laboratories
Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.
Institut Curie
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.
Palacky University
X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement.
Weizmann Institute Of Science
Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmine.
Weizmann Institute Of Science
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
National Institutes Of Health