Journal of Medicinal Chemistry

Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy (Mon, 03 Aug 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00428
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Design, Synthesis, and Characterization of 3-(Benzylidene)indolin-2-one Derivatives as Ligands for α-Synuclein Fibrils (Fri, 31 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00571
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Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors (Fri, 31 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00773
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Tertiary Amine Pyrazolones and Their Salts as Inhibitors of Mutant Superoxide Dismutase 1-Dependent Protein Aggregation for the Treatment of Amyotrophic Lateral Sclerosis (Fri, 31 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00561
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Design, Synthesis, and Biological Evaluation of a Series of Anthracene-9,10-dione Dioxime β-Catenin Pathway Inhibitors (Fri, 31 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00460
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Enantiomerically Pure 2-Methyltetrahydro-3-benzazepin-1-ols Selectively Blocking GluN2B Subunit Containing N-Methyl-d-aspartate Receptors (Thu, 30 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00897
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Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2 (Thu, 30 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00529
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α,β-Methylene-ADP (AOPCP) Derivatives and Analogues: Development of Potent and Selective ecto-5′-Nucleotidase (CD73) Inhibitors (Thu, 30 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00802
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Correction to Design, Synthesis, and Antitumor Evaluation of Novel Histone Deacetylase Inhibitors Equipped with a Phenylsulfonylfuroxan Module as a Nitric Oxide Donor (Thu, 30 Jul 2015)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01075
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Correction to Approved Drugs Containing Thiols as Inhibitors of Metallo-β-lactamases: Strategy To Combat Multidrug-Resistant Bacteria (Thu, 30 Jul 2015)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01097
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A New Class of Potent N-Methyl-d-Aspartate Receptor Inhibitors: Sulfated Neuroactive Steroids with Lipophilic D-Ring Modifications (Wed, 29 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00570
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Synthesis and in Vivo Evaluation of [123I]Melanin-Targeted Agents (Wed, 29 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00777
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Adjusting the DNA Interaction and Anticancer Activity of Pt(II) N-Heterocyclic Carbene Complexes by Steric Shielding of the Trans Leaving Group (Wed, 29 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00896
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A Selective, Cell-Permeable Nonphosphorylated Bicyclic Peptidyl Inhibitor against Peptidyl–Prolyl Isomerase Pin1 (Tue, 28 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00411
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Synthesis of Thrombolytic Sol–Gel Coatings: Toward Drug-Entrapped Vascular Grafts (Tue, 28 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00654
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Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors (Tue, 28 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00788
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Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides (Tue, 28 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00689
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Correction to Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13 (Mon, 27 Jul 2015)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00962
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Novel Levetiracetam Derivatives That Are Effective against the Alzheimer-like Phenotype in Mice: Synthesis, in Vitro, ex Vivo, and in Vivo Efficacy Studies (Mon, 27 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00624
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Development of Fluorine-18 Labeled Metabolically Activated Tracers for Imaging of Drug Efflux Transporters with Positron Emission Tomography (Fri, 24 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00652
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Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) (Fri, 24 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00577
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Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones: Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914) (Fri, 24 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00863
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High Affinity Dopamine D3 Receptor (D3R)-Selective Antagonists Attenuate Heroin Self-Administration in Wild-Type but not D3R Knockout Mice (Thu, 23 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00776
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Distinct Temporal Fingerprint for Cyclic Adenosine Monophosphate (cAMP) Signaling of Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid Receptors (Thu, 23 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00579
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Antibody–Drug Conjugates and Small Molecule–Drug Conjugates: Opportunities and Challenges for the Development of Selective Anticancer Cytotoxic Agents (Thu, 23 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00457
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Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor (Thu, 23 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00227
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Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy (Thu, 23 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00511
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Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4 (Thu, 23 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00226
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Structural Requirements for CNS Active Opioid Glycopeptides (Thu, 23 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00014
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Applications of Fluorine in Medicinal Chemistry (Wed, 22 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00258
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Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma (Wed, 22 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00741
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Structure–Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid (Wed, 22 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00750
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Cyclometalated Iminophosphorane Gold(III) and Platinum(II) Complexes. A Highly Permeable Cationic Platinum(II) Compound with Promising Anticancer Properties (Wed, 22 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00427
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Nucleoside Diphosphate Prodrugs: Nonsymmetric DiPPro-Nucleotides (Wed, 22 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00737
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Development of Safe and Effective Botanical Dietary Supplements (Tue, 21 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00417
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Biological Efficacy and Toxicity of Diamidines in Myotonic Dystrophy Type 1 Models (Tue, 21 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00356
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New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer (Mon, 20 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00310
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Structure–Affinity Relationships (SARs) and Structure–Kinetics Relationships (SKRs) of Kv11.1 Blockers (Fri, 17 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00518
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Structure–Activity Relationship Studies of Substituted 2-(Isoxazol-3-yl)-2-oxo-N′-phenyl-acetohydrazonoyl Cyanide Analogues: Identification of Potent Exchange Proteins Directly Activated by cAMP (EPAC) Antagonists (Thu, 16 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00635
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Discovery and Optimization of a Porcupine Inhibitor (Thu, 16 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00507
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N-Phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATP Competitive DNA Gyrase B Inhibitors: Design, Synthesis, and Evaluation (Wed, 15 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00775
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Discovery of Novel Indazole Derivatives as Highly Potent and Selective Human β3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects (Wed, 15 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00638
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Discovery of CREBBP Bromodomain Inhibitors by High-Throughput Docking and Hit Optimization Guided by Molecular Dynamics (Wed, 15 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00171
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Fragment-Based Design of Selective Nanomolar Ligands of the CREBBP Bromodomain (Wed, 15 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00172
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DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites (Fri, 10 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00150
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Regulation of the Apelinergic System and Its Potential in Cardiovascular Disease: Peptides and Small Molecules as Tools for Discovery (Fri, 10 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00527
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Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor (Mon, 06 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00405
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The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits (Thu, 02 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00313
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Therapeutic Potential of 5-HT6 Receptor Agonists (Thu, 02 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00179
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Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators (Wed, 01 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00229
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Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women’s Health (Fri, 12 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00386
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Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators (Wed, 03 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00516
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Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors (Tue, 26 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00326
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Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00458
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Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications (Thu, 14 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501981g
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Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors (Thu, 14 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00261
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New Frontiers in Selective Human MAO-B Inhibitors (Mon, 11 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501690r
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Ligand Binding Thermodynamics in Drug Discovery: Still a Hot Tip? (Mon, 11 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501511f
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Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition (Thu, 30 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00256
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Activation of the γ-Aminobutyric Acid Type B (GABAB) Receptor by Agonists and Positive Allosteric Modulators (Fri, 24 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5018913
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Progress Toward the Development of Noscapine and Derivatives as Anticancer Agents (Thu, 16 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501180v
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Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B (Mon, 06 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00209
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Volume of Distribution in Drug Design (Wed, 01 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00201
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