145 articles for thisTarget
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Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
Replacing the terminal piperidine in ceritinib with aliphatic amines confers activities against crizotinib-resistant mutants including G1202R.
Korea Research Institute Of Chemical Technology
Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors.
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1.
Shenyang Pharmaceutical University
Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core.
Ocean University Of China
Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
Teva Branded Pharmaceutical Products R & D
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.
Chinese Academy Of Sciences
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Ariad Pharmaceuticals
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.
Southeast University
Pyrazolylamine Derivatives Reveal the Conformational Switching between Type I and Type II Binding Modes of Anaplastic Lymphoma Kinase (ALK).
National Health Research Institutes
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.
Zhejiang University
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.
Nerviano Medical Sciences
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).
Green Valley Research Institute
Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.
Korea Research Institute Of Chemical Technology
Novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety against anaplastic lymphoma kinase (ALK): Synthesis, in vitro, ex vivo, and in vivo efficacy studies.
Chungbuk National University
Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Beijing Pearl Biotech
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
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
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.
Hanyang University
Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor.
Korea Research Institute Of Chemical Technology
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Beijing Pearl Biotech
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.
Nerviano Medical Sciences
Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.
Teva Branded Pharmaceutical Products R & D
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Genomics Institute Of The Novartis Research Foundation
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.
University Of South Florida
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.
Chinese Academy Of Sciences
Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors.
Korea University Of Science And Technology
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
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Zhejiang University
Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Shanghai Institute Of Materia Medica (Simm)
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.
Qilu Pharmaceutical
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expo
Pfizer
Syk inhibitors with high potency in presence of blood.
Novartis Institutes For Biomedical Research
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities.
State Key Laboratory Of Drug Research
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.
Martin-Luther-University Halle-Wittenberg
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Pfizer
Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors.
Universit£
Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.
Heinrich Heine Universit£T
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
Heinrich-Heine-Universit£T D£Sseldorf
Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors.
Korea Research Institute Of Chemical Technology
Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors.
Southern Medical University
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.
Chugai Pharmaceutical
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
Discovery of 7-azaindole based anaplastic lymphoma kinase (ALK) inhibitors: wild type and mutant (L1196M) active compounds with unique binding mode.
Aurigene Discovery Technologies
LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor.
University Of Michigan Comprehensive Cancer Center
Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases.
Osi Pharmaceuticals
Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.
Novartis Institutes For Biomedical Research
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase
Genomics Institute Of The Novartis Research Foundation
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.
Sichuan University
The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
Amgen
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.
Cephalon
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
TBA
Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.
TBA
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
Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.
Amgen
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Abbott Laboratories
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c
Cephalon
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.
Hanyang University
4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.
Nerviano Medical Sciences
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.
Nerviano Medical Sciences Oncology
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Cephalon
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
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.
University Of Milano-Bicocca
Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.
Glaxosmithkline
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.1³,¿?¿.1¿?¿,¹³]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles.
Cephalon
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
Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors.
TBA
Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).
Chugai Pharmaceutical
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.
Cephalon
2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.
Cephalon
9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.
Peking University
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
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
2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.
Cephalon
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
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
Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.
Heinrich Heine Universit£T
Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.
St. Jude Children'S Research Hospital
Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.
Cephalon
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.
Pfizer
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
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
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.
Cephalon
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.
Novartis Institutes For Biomedical Research
Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factorß receptor I (TGFßRI).
Boehringer Ingelheim Pharma
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.
Technische Universit£T Braunschweig
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Novartis Institute Of Biomedical Research
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
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
Vertex Pharmaceuticals
Design and synthesis of a novel tyrosine kinase inhibitor template.
St. Jude Children'S Research Hospital
Identification of novel protein kinase CK1 delta (CK1delta) inhibitors through structure-based virtual screening.
Università
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Genomics Institute Of The Novartis Research Foundation
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.
University Of Milano-Bicocca
Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.
Università
Design and synthesis of 5-aryl-pyridone-carboxamides as inhibitors of anaplastic lymphoma kinase.
Chembridge Research Laboratories And Chembridge
Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization.
Shanghai Pharmaceuticals Holding
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
Novel 2,4-diaminopyrimidines bearing fused tricyclic ring moiety for anaplastic lymphoma kinase (ALK) inhibitor.
University Of Science & Technology
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis.
Centre De Recherche De Gif
Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.
China Pharmaceutical University
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.
Aimst University
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
Gsk
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Merck Research Laboratories
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.
Abbott Laboratories
Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: synthesis and biological evaluation.
Cardiff University
4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2.
University Of Newcastle
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.
University Of Newcastle
DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORS
Parke-Davis Pharmaceutical Research