Journal of Medicinal Chemistry

[ASAP] DDX3X Helicase Inhibitors as a New Strategy To Fight the West Nile Virus Infection (Thu, 21 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01403
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[ASAP] Medical Uses of Silver: History, Myths, and Scientific Evidence (Thu, 21 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01439
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[ASAP] Targeting the MKK7–JNK (Mitogen-Activated Protein Kinase Kinase 7–c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors (Thu, 21 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00102
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[ASAP] Determination of Ligand Binding Epitope Structures Using Polarization Transfer from Hyperpolarized Ligands (Wed, 20 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01711
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[ASAP] Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles (Wed, 20 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01729
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[ASAP] Development of an <italic toggle="yes">N</italic>-Acyl Amino Acid That Selectively Inhibits the Glycine Transporter 2 To Produce Analgesia in a Rat Model of Chronic Pain (Wed, 20 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01775
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[ASAP] Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma (Wed, 20 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01857
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[ASAP] 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site (Mon, 18 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01766
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[ASAP] 3,17ß-Bis-sulfamoyloxy-2-methoxyestra-1,3,5(10)-triene and Nonsteroidal Sulfamate Derivatives Inhibit Carbonic Anhydrase IX: Structure–Activity Optimization for Isoform Selectivity (Mon, 18 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01990
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[ASAP] 6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors (Sat, 16 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01726
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[ASAP] Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Ia and d (Fri, 15 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01541
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[ASAP] Tigliane Diterpenoids as a New Type of Antiadipogenic Agents Inhibit GRa-Dexras1 Axis in Adipocytes (Fri, 15 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01693
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[ASAP] Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation (Fri, 15 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01848
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[ASAP] Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides (Fri, 15 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01908
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[ASAP] New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective (<italic toggle="yes">Z</italic>)-<italic toggle="yes">N</italic>-<italic toggle="yes">tert</italic>-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment (Fri, 15 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01987
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[ASAP] Synthesis and Structural/Functional Characterization of Selective M14 Metallocarboxypeptidase Inhibitors Based on Phosphinic Pseudopeptide Scaffold: Implications on the Design of Specific Optical Probes (Wed, 13 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01465
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[ASAP] Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes (Wed, 13 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01491
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[ASAP] Photoactivatable Prodrug of Doxazolidine Targeting Exosomes (Wed, 13 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01508
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[ASAP] Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140) (Wed, 13 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01679
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[ASAP] Phenolic Bis-styrylbenzo[<italic toggle="yes">c</italic>]-1,2,5-thiadiazoles as Probes for Fluorescence Microscopy Mapping of Aß Plaque Heterogeneity (Wed, 13 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01681
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[ASAP] 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action (Wed, 13 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01765
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[ASAP] Effects of Systematic Shortening of Noncovalent C8 Side Chain on the Cytotoxicity and NF-?B Inhibitory Capacity of Pyrrolobenzodiazepines (PBDs) (Wed, 13 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01849
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[ASAP] Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs) (Tue, 12 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01520
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[ASAP] Absolute Binding Free Energy Calculation and Design of a Subnanomolar Inhibitor of Phosphodiesterase-10 (Tue, 12 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01763
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[ASAP] Deciphering the Role of Intramolecular Networking in Cholic Acid–Peptide Conjugates on the Lipopolysaccharide Surface in Combating Gram-Negative Bacterial Infections (Mon, 11 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01357
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[ASAP] Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor (Mon, 11 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01483
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[ASAP] Identification and Optimization of Novel Small c-Abl Kinase Activators Using Fragment and HTS Methodologies (Mon, 11 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01872
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[ASAP] New Rigid Nicotine Analogues, Carrying a Norbornane Moiety, Are Potent Agonists of a7 and a3* Nicotinic Receptors (Fri, 08 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01372
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[ASAP] Small-Molecule Modulators of the Hypoxia-Inducible Factor Pathway: Development and Therapeutic Applications (Fri, 08 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01596
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[ASAP] Crown Ethers as Transthyretin Amyloidogenesis Inhibitors (Fri, 08 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01700
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[ASAP] Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors (Fri, 08 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01725
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[ASAP] Correction to Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na<sub>V</sub>1.7 Inhibitors for the Treatment of Pain (Fri, 08 Feb 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00202
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[ASAP] Discovery of a Series of 2'-a-Fluoro,2'-ß-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus (Thu, 07 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01300
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[ASAP] Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPAR? Drug Pioglitazone (Thu, 07 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01573
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[ASAP] Discovery of Macrocyclic Inhibitors of Apurinic/Apyrimidinic Endonuclease 1 (Wed, 06 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01529
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[ASAP] Selective Targeting of Integrin avß8 by a Highly Active Cyclic Peptide (Wed, 06 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01588
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[ASAP] Discovery of Potent, Selective, and Orally Bioavailable Estrogen-Related Receptor-? Inverse Agonists To Restore the Sodium Iodide Symporter Function in Anaplastic Thyroid Cancer (Mon, 04 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01296
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[ASAP] Substrate-Specific Inhibition Constants for Phospholipase A<sub>2</sub> Acting on Unique Phospholipid Substrates in Mixed Micelles and Membranes Using Lipidomics (Mon, 04 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01568
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[ASAP] Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives (Fri, 01 Feb 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01668
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[ASAP] Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology (Fri, 25 Jan 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01153
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[ASAP] Applications of Deuterium in Medicinal Chemistry (Fri, 25 Jan 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01808
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[ASAP] Development of Isoselenocyanate Compounds’ Syntheses and Biological Applications (Tue, 22 Jan 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01698
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[ASAP] Drug Annotations Series Change in Guidelines (Tue, 22 Jan 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00038
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[ASAP] In Search of GABA<sub>A</sub> Receptor’s Neurosteroid Binding Sites<subtitle>Miniperspective</subtitle> (Mon, 31 Dec 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01400
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[ASAP] The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic (Thu, 27 Dec 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00843
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[ASAP] Evolution of PI3K? and d Inhibitors for Inflammatory and Autoimmune Diseases (Mon, 24 Dec 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01298
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[ASAP] Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective (Mon, 24 Dec 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01492
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[ASAP] 1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation (Fri, 21 Dec 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01386
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[ASAP] Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update (Thu, 20 Dec 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01469
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[ASAP] Polymethine Thiopyrylium Fluorophores with Absorption beyond 1000 nm for Biological Imaging in the Second Near-Infrared Subwindow (Thu, 13 Dec 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01682
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