PMID

Data

Article Title

Organization

Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors.

Hamdard University

Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.

Peking University

Design of a doxorubicin-peptidomimetic conjugate that targets HER2-positive cancer cells.

University Of Louisiana At Monroe

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck

Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.

Tsinghua 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

Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.

University Of Auckland

Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.

China Pharmaceutical University

Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.

East China University Of Science & Technology

Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor.

Southern Medical University

An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.

Chinese Academy Of Sciences

6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR.

Zhejiang University

Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.

Southeast University

Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.

Harvard Medical School

Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation.

Astrazeneca

Sequential one-pot synthesis of bis(indolyl)glyoxylamides: Evaluation of antibacterial and anticancer activities.

Birla Institute Of Technology

Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.

Oribase Pharma

Discovery of new [1,4]dioxino[2,3-f]quinazoline-based inhibitors of EGFR including the T790M/L858R mutant.

Beijing University Of Technology

Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors.

Fudan University

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

Recent progress on third generation covalent EGFR inhibitors.

Pfizer

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.

Pfizer

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

Genentech

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research

Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors.

Beijing University Of Technology

Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines.

Dalian Medical University

Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.

Chinese Academy Of Sciences

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.

Genentech

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

Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.

Nanjing University

Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.

Korea University Of Science And Technology (Ust)

Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.

Amgen

Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.

Sichuan University

Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.

Astrazeneca

Design, synthesis and molecular modeling of biquinoline-pyridine hybrids as a new class of potential EGFR and HER-2 kinase inhibitors.

Nanjing University

Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.

Christian-Albrechts-University Of Kiel

Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.

Astellas Pharma

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.

Technische Universit£T Dortmund

Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.

Chinese Academy Of Sciences

Recent advances in the chemistry and biology of pyridopyrimidines.

Universit£

Computer-aided identification of novel anticancer compounds with a possible dual HER1/HER2 inhibition mechanism.

Cardiff University

A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.

Zhejiang University

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.

Genentech

Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.

Southeast University

Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.

Astrazeneca

Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.

Peking University

Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.

Chinese Academy Of Sciences

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

Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.

Takeda Pharmaceutical

Structure-based discovery of cellular-active allosteric inhibitors of FAK.

Takeda Pharmaceutical

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

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

Fluorescence study for selecting specific ligands toward HER2 receptor: an example of receptor fragment approach.

Institute Of Biostructures And Bioimages

Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents.

Nanjing University

Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives containing benzodioxole as potential anticancer agents.

Nanjing University

1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.

Glaxosmithkline

N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.

Glaxosmithkline

Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.

University Of Tennessee Health Sciences Center

Irreversible protein kinase inhibitors: balancing the benefits and risks.

Covalution Pharma

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Abbott Laboratories

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

Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research And Development

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

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

Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents.

Nanjing University

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

Discovery of 6-substituted 4-anilinoquinazolines with dioxygenated rings as novel EGFR tyrosine kinase inhibitors.

Nanjing University

A fluorescent reporter of ATP binding-competent receptor kinases.

University Of Miami

Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.

Chinese Academy Of Sciences

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

Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides.

Universit£

Synthesis, molecular modeling, and biological evaluation of cinnamic acid metronidazole ester derivatives as novel anticancer agents.

Nanjing University

Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.

Chinese Academy Of Sciences

Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.

Incyte

Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.

Bristol-Myers Squibb Research And Development

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.

University Of South Florida

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

Discovery and development of heat shock protein 90 inhibitors.

Memorial Sloan-Kettering Cancer Center

Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.

Glaxosmithkline

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

Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.

Johnson & Johnson Pharmaceutical Research & Development

Formation of fluorine-18 labeled diaryl ureas--labeled VEGFR-2/PDGFR dual inhibitors as molecular imaging agents for angiogenesis.

Hadassah Hebrew University Hospital

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University Of Oxford

Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.

Astrazeneca

A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Astrazeneca

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

Anilinodialkoxyquinazolines: screening epidermal growth factor receptor tyrosine kinase inhibitors for potential tumor imaging probes.

Lawrence Berkeley National Laboratory

Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.

Glaxosmithkline

Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.

Pfizer

Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.

Wyeth Research

Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).

Wyeth Research

Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.

Wyeth Research

 

Indolocarbazoles. 1. Total synthesis and protein kinase inhibiting characteristics of compounds related to K-252c.

TBA

Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.

Westf£Lische Wilhelms-Universit£T M£Nster

Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors.

Nanjing University

Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.

Glaxosmithkline

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

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

Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.

East China University Of Science And Technology

Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.

University Of Regensburg

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

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

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

Metronidazole acid acyl sulfonamide: a novel class of anticancer agents and potential EGFR tyrosine kinase inhibitors.

Nanjing University

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

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 pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.

Bristol-Myers Squibb

Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.

Chugai Pharmaceutical

Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.

Chinese Academy Of Sciences

Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.

Shionogi

Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277

TBA

Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Research And Development

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

Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.

Abbott Laboratories

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

Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.

Temple University School Of Medicine

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

Phage-encoded combinatorial chemical libraries based on bicyclic peptides.

Laboratory Of Molecular Biology, Medical Research Council

BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.

Boehringer Ingelheim Austria

Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.

Southeast University

New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.

Novartis Institute Of Biomedical Research

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

Selectively nonselective kinase inhibition: striking the right balance.

Schering-Plough

Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.

Shanghai Hengrui Pharmaceuticals

Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.

Hadassah Hebrew University Hospital

Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents.

Nanjing University

Synthesis and structure-activity relationships of N-benzyl-N-(X-2-hydroxybenzyl)-N'-phenylureas and thioureas as antitumor agents.

Nanjing University

Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors.

Nanjing University

Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.

Curis

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.

4Sc

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

Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.

Glaxosmithkline

 

Inhibition of the her2 tyrosine kinase and characterization of a hydrophobic site near the nucleotide binding domain

TBA

Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

Incyte

N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.

4Sc

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).

Glaxosmithkline

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

The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.

Glaxosmithkline

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

Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.

The Scripps Research Institute

4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors.

Johnson & Johnson Pharmaceutical Research And Development

Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening.

Institute Of Materia Medica

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 characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors.

Eberhard-Karls University

Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach.

University Of Southern California

Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.

Freie UniversitäT Berlin

Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Astrazeneca

Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.

Bristol-Myers Squibb Research And Development

Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Astrazeneca

5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.

Johnson & Johnson Pharmaceutical Research & Development

Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.

Johnson & Johnson Pharmaceutical Research & Development

The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.

Pfizer

Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute

New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

Incyte

Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase.

Sun Yat-Sen University

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

Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.

Glaxosmithkline

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

The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR).

Mcgill University Health Center/Royal Victoria Hospital

High-throughput screening for Hsp90 ATPase inhibitors.

The University Of Kansas

Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.

Glaxosmithkline

(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

Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.

Novartis Institutes For Biomedical Research

Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.

Bristol-Myers Squibb

New dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute

High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors.

Hadassah Hebrew University

5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.

Astrazeneca

Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.

Glaxosmithkline

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

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

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.

Novartis Institutes For Biomedical Research

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

Bristol-Myers Squibb Pharmaceutical Research Institute

Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold.

Institut FüR Molekulare Physiologie

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.

Boehringer Ingelheim Pharmaceuticals

Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.

Bayer Research Center

Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.

Jiangsu Aosaikang Pharmaceutical

Disabling erbB receptors with rationally designed exocyclic mimetics of antibodies: structure-function analysis.

University Of Pennsylvania School Of Medicine

Potent dual EGFR/Her4 tyrosine kinase inhibitors containing novel (1,2-dithiolan-4-yl)acetamides.

Sabila Biosciences

Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.

Research Biomet. Glaxo Wellcome Medicines Research Centre

Acetylene Group, Friend or Foe in Medicinal Chemistry.

St. John'S University

New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.

Universidad San Pablo-Ceu

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.

Merck

Discovery of N-(benzyloxy)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives as potential antiproliferative agents by inhibiting MEK.

Anhui Agricultural University

Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And

Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors.

Mansoura University

Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs.

Jiangsu Aosaikang Pharmaceutical

Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.

University Of Auckland

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.

TBA

CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.

Shaoxing University

Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors.

Anadolu University

Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.

University Of Oregon

Estrogen signaling: An emanating therapeutic target for breast cancer treatment.

Indian Institute Of Technology (Bhu)

Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.

Sabila Biosciences

Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.

University Of Auckland

Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.

Chinese Academy Of Sciences

Discovery of a potent dual ALK and EGFR T790M inhibitor.

Harvard Medical School

Discovery of 4

TBA

Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.

Chung-Ang University

Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.

TBA

The Exploration of Chirality for Improved Druggability within the Human Kinome.

University Of Arkansas For Medical Sciences

Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.

Eberhard Karls University T£Bingen

Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.

Sichuan University And Collaborative Innovation Center

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

Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.

Arromax Pharmatech

Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.

University Of Naples Federico Ii

Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.

Southeast University

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.

Qingdao University

Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1.

Arromax Pharmatech

The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.

University Of South China

Discovery of N

Zhuhai Campus Of Zunyi Medical University

Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.

Beijing University Of Chemical Technology

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

Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases.

Warner-Lambert

Discovery and Development of a Series of Pyrazolo[3,4-

Shanghai University

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.

Pfizer

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

Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents.

Xi'An Jiaotong University

Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.

Abbvie Bioresearch Center

Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant.

Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.

Argenta Discovery

Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.

Xavier University Of Louisiana

Recycling antimalarial leads for cancer: Antiproliferative properties of N-cinnamoyl chloroquine analogues.

Centro De Investiga££O Em Qu£Mica Da Universidade Do Porto

Design, synthesis, and biological evaluation of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible epidermal growth factor receptor inhibitors with improved pharmacokinetic properties.

Chinese Academy Of Sciences

Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer.

Qilu Pharmaceutical

Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant.

East China University Of Science & Technology

5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.

Sterling Winthrop Pharmaceuticals Research Division

Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).

Astrazeneca

Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins.

Hebrew University Of Jerusalem

Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors.

Chinese Academy Of Sciences

Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer.

China Pharmaceutical University

Inhibitory effects of metachromins L-Q and its related analogs against receptor tyrosine kinases EGFR and HER2.

Hokkaido University

Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium.

Heinrich-Heine-Universitat

Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense.

Heinrich-Heine-Universit£T

Spongiacidins A-D, new bromopyrrole alkaloids from hymeniacidon sponge

Hokkaido University

Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.

Al-Azhar University

Surmounting the resistance against EGFR inhibitors through the development of thieno[2,3-d]pyrimidine-based dual EGFR/HER2 inhibitors.

Ain Shams University

Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors.

Chinese Academy Of Sciences

How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.

Ain Shams University

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.

Pfizer

Design of novel lipidated peptidomimetic conjugates for targeting EGFR heterodimerization in HER2?+?cancer.

University Of Louisiana At Monroe

Success stories of natural product-based hybrid molecules for multi-factorial diseases.

Punjabi University

Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.

Universit£

Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.

China Pharmaceutical University

Discovery of new erbB4 inhibitors: Repositioning an orphan chemical library by inverse virtual screening.

University Of Salerno

Design and synthesis of bis(indolyl)ketohydrazide-hydrazones: Identification of potent and selective novel tubulin inhibitors.

Birla Institute Of Technology

Discovery of Benzo[g]quinazolin benzenesulfonamide derivatives as dual EGFR/HER2 inhibitors.

King Saud University

Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.

Sichuan University And Collaborative Innovation Center

Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.

High Magnetic Field Laboratory

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

Trimethylation of histone H3 lysine 36 by human methyltransferase PRDM9 protein.

University Of Toronto

Synthesis and in vitro activity of heterocyclic inhibitors of CYP2A6 and CYP2A13, two cytochrome P450 enzymes present in the respiratory tract.

University Of Basel

Crystal structure analysis and in silico pKa calculations suggest strong pKa shifts of ligands as driving force for high-affinity binding to TGT.

Philipps-UniversitÄT Marburg

Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.

Wyeth Research

RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information.

Gilead Sciences

Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.

Pfizer

Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis.

Universita Degli Studi

Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase.

Pfizer

Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.

Griffith University

A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera.

Astex

Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.

University Of Michigan

Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.

Smithkline Beecham Pharmaceuticals

Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor.

University Of Auckland