Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis
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Title
Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis
Authors
Keywords
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Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 65, Issue 2, Pages 1047-1131
Publisher
American Chemical Society (ACS)
Online
2021-10-10
DOI
10.1021/acs.jmedchem.1c00963
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- Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes
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- Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs
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- Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases
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- 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 Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations
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- Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634
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- Docetaxel plus nintedanib versus docetaxel plus placebo in patients with previously treated non-small-cell lung cancer (LUME-Lung 1): a phase 3, double-blind, randomised controlled trial
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- Alectinib Shows Potent Antitumor Activity against RET-Rearranged Non-Small Cell Lung Cancer
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- Characterization of the Novel and Specific PI3K Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials
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- A novel approach for the synthesis of Crizotinib through the key chiral alcohol intermediate by asymmetric hydrogenation using highly active Ir-Spiro-PAP catalyst
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- Distinct Binding Mode of Multikinase Inhibitor Lenvatinib Revealed by Biochemical Characterization
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- AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer
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- The ALK Inhibitor Ceritinib Overcomes Crizotinib Resistance in Non-Small Cell Lung Cancer
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- Phase 2 Randomized Clinical Study of a Rho Kinase Inhibitor, K-115, in Primary Open-Angle Glaucoma and Ocular Hypertension
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- Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseases
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- Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
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- Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants
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- PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Responses and Suppresses Activity in Autoimmune and Inflammatory Disease Models
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- A Critical Review of Trials of First-Line BCR-ABL Inhibitor Treatment in Patients With Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase
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- A randomised, double-blind phase III study of pazopanib in patients with advanced and/or metastatic renal cell carcinoma: Final overall survival results and safety update
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- Tivozanib Versus Sorafenib As Initial Targeted Therapy for Patients With Metastatic Renal Cell Carcinoma: Results From a Phase III Trial
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- Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)
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- 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 2 Clinical Trials
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- Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial
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- Safety and efficacy of CYT387, a JAK1 and JAK2 inhibitor, in myelofibrosis
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- Targeting BTK with Ibrutinib in Relapsed or Refractory Mantle-Cell Lymphoma
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- Ipilimumab, Vemurafenib, Dabrafenib, and Trametinib: Synergistic Competitors in the Clinical Management of BRAF Mutant Malignant Melanoma
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- The ErbB/HER family of protein-tyrosine kinases and cancer
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- Axitinib for the Management of Metastatic Renal Cell Carcinoma
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- Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors
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- Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets
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- Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial
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- Off-target effects of BCR–ABL1 inhibitors and their potential long-term implications in patients with chronic myeloid leukemia
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- Chemical, genetic and structural assessment of pyridoxal kinase as a drug target in the African trypanosome
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- Comprehensive molecular portraits of human breast tumours
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- Ponatinib in Refractory Philadelphia Chromosome–Positive Leukemias
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- Placebo-Controlled Trial of Tofacitinib Monotherapy in Rheumatoid Arthritis
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- The synthesis of Bcr-Abl inhibiting anticancer pharmaceutical agents imatinib, nilotinib and dasatinib
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- CH5424802, a Selective ALK Inhibitor Capable of Blocking the Resistant Gatekeeper Mutant
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- 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
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- Metabolite characterization of a novel anti-cancer agent, icotinib, in humans through liquid chromatography/quadrupole time-of-flight tandem mass spectrometry
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- Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate)
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- Creating Diverse Target-Binding Surfaces on FKBP12: Synthesis and Evaluation of a Rapamycin Analogue Library
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