Title: 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.
Journal: Journal of medicinal chemistry 20160908
Title: Phase I study of temsirolimus in combination with EKB-569 in patients with advanced solid tumors.
Journal: Investigational new drugs 20121001
Title: Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance.
Journal: Biochemical pharmacology 20120801
Title: Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: therapeutic implications.
Journal: International journal of cancer 20120701
Title: Novel EGFR-TK inhibitor EKB-569 inhibits hepatocellular carcinoma cell proliferation by AKT and MAPK pathways.
Journal: Journal of Korean medical science 20111201
Title: The PI3 kinase/mTOR blocker NVP-BEZ235 overrides resistance against irreversible ErbB inhibitors in breast cancer cells.
Journal: Breast cancer research and treatment 20110901
Title: Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
Journal: European journal of medicinal chemistry 20110601
Title: Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.
Journal: Journal of medicinal chemistry 20110310
Title: Irreversible EGFR inhibitor EKB-569 targets low-LET γ-radiation-triggered rel orchestration and potentiates cell death in squamous cell carcinoma.
Journal: PloS one 20110101
Title: Development of a new epidermal growth factor receptor positron emission tomography imaging agent based on the 3-cyanoquinoline core: synthesis and biological evaluation.
Journal: Bioorganic & medicinal chemistry 20100915
Title: Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions.
Journal: Cancer treatment reviews 20091201
Title: A phase I study of EKB-569 in combination with capecitabine in patients with advanced colorectal cancer.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080901
Title: Redesigning kinase inhibitors to enhance specificity.
Journal: Journal of medicinal chemistry 20080828
Title: The development of HKI-272 and related compounds for the treatment of cancer.
Journal: Archiv der Pharmazie 20080801
Title: Chronic pharmacologic inhibition of EGFR leads to cardiac dysfunction in C57BL/6J mice.
Journal: Toxicology and applied pharmacology 20080501
Title: Towards predictive inhibitor design for the EGFR autophosphorylation activity.
Journal: European journal of medicinal chemistry 20080401
Title: Phase I pharmacokinetic/pharmacodynamic study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor tyrosine kinase, in combination with irinotecan, 5-fluorouracil, and leucovorin (FOLFIRI) in first-line treatment of patients with metastatic colorectal cancer.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080101
Title: A quantitative analysis of kinase inhibitor selectivity.
Journal: Nature biotechnology 20080101
Title: Biochemical assay-based selectivity profiling of clinically relevant kinase inhibitors on mutant forms of EGF receptor.
Journal: Journal of receptor and signal transduction research 20080101
Title: Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
Journal: Bioorganic & medicinal chemistry 20070601
Title: In-Cell Western analysis of Helicobacter pylori-induced phosphorylation of extracellular-signal related kinase via the transactivation of the epidermal growth factor receptor.
Journal: Microbes and infection 20070601
Title: Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer.
Journal: The oncologist 20070301
Title: Pharmacology of epidermal growth factor inhibitors.
Journal: The International journal of biological markers 20070101
Title: Is there a role for the irreversible epidermal growth factor receptor inhibitor EKB-569 in the treatment of cancer? A mutation-driven question.
Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060520
Title: Phase I study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor, in patients with advanced solid tumors.
Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060520
Title: EKB-569, a new irreversible epidermal growth factor receptor tyrosine kinase inhibitor, with clinical activity in patients with non-small cell lung cancer with acquired resistance to gefitinib.
Journal: Lung cancer (Amsterdam, Netherlands) 20060301
Title: Recent developments related to the EGFR as a target for cancer chemotherapy.
Journal: Current opinion in pharmacology 20050801
Title: Small molecules with EGFR-TK inhibitor activity.
Journal: Current drug targets 20050501
Title: A small molecule-kinase interaction map for clinical kinase inhibitors.
Journal: Nature biotechnology 20050301
Title: Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
Journal: Journal of medicinal chemistry 20050224
Title: The epidermal growth factor receptor as a target for colorectal cancer therapy.
Journal: Seminars in oncology 20050201
Title: Epidermal growth factor receptor tyrosine kinase inhibition is not protective in PCK rats.
Journal: Kidney international 20041101
Title: Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles.
Journal: Bioorganic & medicinal chemistry letters 20040322
Title: Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes.
Journal: Molecular cancer therapeutics 20040101
Title: Combination treatment of PKD utilizing dual inhibition of EGF-receptor activity and ligand bioavailability.
Journal: Kidney international 20031001
Title: Clinical studies with non-iressa EGFR tyrosine kinase inhibitors.
Journal: Lung cancer (Amsterdam, Netherlands) 20030801
Title: Developing inhibitors of the epidermal growth factor receptor for cancer treatment.
Journal: Journal of the National Cancer Institute 20030618
Title: 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).
Journal: Journal of medicinal chemistry 20030102
Title: 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.
Journal: Bioorganic & medicinal chemistry letters 20021021
Title: Torrance CJ, et al. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8.
Title: Nunes M, et al. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3(1):21-7.