Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
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Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophoreRedox-directed cancer therapeutics: molecular mechanisms and opportunitiesThe T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATPProfile of neratinib and its potential in the treatment of breast cancerHuman epidermal growth factor receptor family-targeted therapies in the treatment of HER2-overexpressing breast cancerDeveloping irreversible inhibitors of the protein kinase cysteinomeStructures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor SensitivityAGO Recommendations for Diagnosis and Treatment of Patients with Primary and Metastatic Breast Cancer. Update 2011.Phase I study of temsirolimus in combination with EKB-569 in patients with advanced solid tumors.Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinasesStrategies for discovering and derisking covalent, irreversible enzyme inhibitors.A structure-guided approach to creating covalent FGFR inhibitorsSynthesis of alpha-ketoester- and alpha-hydroxyester-substituted isoindazoles via the thermodynamic coarctate cyclization of ester-terminated azo-ene-yne systems.Small-molecule inhibitors of the receptor tyrosine kinases: promising tools for targeted cancer therapiesPresent and future evolution of advanced breast cancer therapy.Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor.Therapeutic strategies and mechanisms of tumorigenesis of HER2-overexpressing breast cancerTargeting the function of the HER2 oncogene in human cancer therapeutics.Characteristics of CD8+ T cell subsets in Chinese patients with chronic HIV infection during initial ART.Pharmacokinetics of oral neratinib during co-administration of ketoconazole in healthy subjectsIn silico identification of EGFR-T790M inhibitors with novel scaffolds: start with extraction of common featuresPreclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2Combining emerging agents in advanced breast cancerTargeted Therapies in Breast Cancer: Implications for Advanced Oncology Practice.N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.Label-free LC-MS analysis of HER2+ breast cancer cell line response to HER2 inhibitor treatment.Discovery of a series of novel phenylpiperazine derivatives as EGFR TK inhibitors.Neratinib reverses ATP-binding cassette B1-mediated chemotherapeutic drug resistance in vitro, in vivo, and ex vivo.Neratinib shows efficacy in the treatment of HER2 amplified carcinosarcoma in vitro and in vivo.Structure-guided design of purine-based probes for selective Nek2 inhibitionEfficacy and mechanism of action of the tyrosine kinase inhibitors gefitinib, lapatinib and neratinib in the treatment of HER2-positive breast cancer: preclinical and clinical evidenceEpidermal growth factor receptor inhibitors in the treatment of non-small cell lung cancer.Cheminfomatic-based Drug Discovery of Human Tyrosine Kinase Inhibitors.Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agentsCombination neratinib (HKI-272) and paclitaxel therapy in patients with HER2-positive metastatic breast cancer.A gene expression profile indicative of early stage HER2 targeted therapy responseOvercoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.Antitumor Activity of TAK-285, an Investigational, Non-Pgp Substrate HER2/EGFR Kinase Inhibitor, in Cultured Tumor Cells, Mouse and Rat Xenograft Tumors, and in an HER2-Positive Brain Metastasis Model.
P2860
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P2860
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
description
2005 nî lūn-bûn
@nan
2005年の論文
@ja
2005年論文
@yue
2005年論文
@zh-hant
2005年論文
@zh-hk
2005年論文
@zh-mo
2005年論文
@zh-tw
2005年论文
@wuu
2005年论文
@zh
2005年论文
@zh-cn
name
Optimization of 6,7-disubstitu ...... or receptor-2 kinase activity.
@en
type
label
Optimization of 6,7-disubstitu ...... or receptor-2 kinase activity.
@en
prefLabel
Optimization of 6,7-disubstitu ...... or receptor-2 kinase activity.
@en
P2093
P356
P1476
Optimization of 6,7-disubstitu ...... or receptor-2 kinase activity.
@en
P2093
Allan Wissner
Bernard D Johnson
Carolyn Discafani
Elsebe G Overbeek-Klumpers
Hwei-Ru Tsou
Janis Upeslacis
Jonathan Golas
M Brawner Floyd
Marvin F Reich
Ramaswamy Nilakantan
P304
P356
10.1021/JM040159C
P407
P577
2005-02-01T00:00:00Z