Journal of Medicinal Chemistry

Discovery of Selective Small-Molecule Inhibitors for the β-Catenin/T-Cell Factor Protein–Protein Interaction through the Optimization of the Acyl Hydrazone Moiety (Fri, 22 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00223
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Privileged Structures Meet Human T-Cell Leukemia Virus-1 (HTLV-1): C2-Symmetric 3,4-Disubstituted Pyrrolidines as Nonpeptidic HTLV-1 Protease Inhibitors (Fri, 22 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00346
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Combining Active Immunization with Monoclonal Antibody Therapy To Facilitate Early Initiation of a Long-Acting Anti-Methamphetamine Antibody Response (Fri, 22 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00220
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Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts (Fri, 22 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00054
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Structure–Activity Relationship and Pharmacokinetic Studies of 1,5-Diheteroarylpenta-1,4-dien-3-ones: A Class of Promising Curcumin-Based Anticancer Agents (Fri, 22 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00470
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Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist (Fri, 22 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00217
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Structure–Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors (Thu, 21 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00407
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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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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00393
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Differential Targeting of Human Topoisomerase II Isoforms with Small Molecules (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00473
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Design, Synthesis, and Biological Evaluation of Hexacyclic Tetracyclines as Potent, Broad Spectrum Antibacterial Agents (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00262
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Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00140
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Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501840b
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Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00128
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Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00330
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A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides (Tue, 19 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00114
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Cyclopentadienyl–Ruthenium(II) and Iron(II) Organometallic Compounds with Carbohydrate Derivative Ligands as Good Colorectal Anticancer Agents (Fri, 15 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00403
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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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The Discovery and Characterization of the α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Potentiator N-{(3S,4S)-4-[4-(5-Cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242) (Thu, 14 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00300
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Discovery of a High Affinity and Selective Pyridine Analog as a Potential Positron Emission Tomography Imaging Agent for Cannabinoid Type 2 Receptor (Thu, 14 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00283
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First Crystal Structures of Mycobacterium tuberculosis 6-Oxopurine Phosphoribosyltransferase: Complexes with GMP and Pyrophosphate and with Acyclic Nucleoside Phosphonates Whose Prodrugs Have Antituberculosis Activity (Wed, 13 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00611
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Structure–Activity Relationships of Lysophosphatidylserine Analogs as Agonists of G-Protein-Coupled Receptors GPR34, P2Y10, and GPR174 (Wed, 13 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5020082
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Discovery of 1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a Pan-RAF Inhibitor with Minimal Paradoxical Activation and Activity against BRAF or RAS Mutant Tumor Cells (Tue, 12 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00067
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Synthesis and Evaluation of 1,2,4-Triazolo[1,5-a]pyrimidines as Antibacterial Agents Against Enterococcus faecium (Tue, 12 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501831g
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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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Methyl 3-((6-Methoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)amino)benzoate (GN39482) as a Tubulin Polymerization Inhibitor Identified by MorphoBase and ChemProteoBase Profiling Methods (Mon, 11 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00035
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Correlating Molecular Character of NIR Imaging Agents with Tissue-Specific Uptake (Fri, 08 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00475
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Design of Highly Potent Urea-Based, Exosite-Binding Inhibitors Selective for Glutamate Carboxypeptidase II (Thu, 07 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00278
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Design, Synthesis, and Antitumor Evaluation of Novel Histone Deacetylase Inhibitors Equipped with a Phenylsulfonylfuroxan Module as a Nitric Oxide Donor (Thu, 07 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00317
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Improving the Pharmacokinetic and CYP Inhibition Profiles of Azaxanthene-Based Glucocorticoid Receptor ModulatorsIdentification of (S)-5-(2-(9-Fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5H-chromeno[2,3-b]pyridin-5-yl)-2-methylpropanamido)-N-(tetrahydro-2H-pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide (BMS-341) (Thu, 07 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00257
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Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor (Thu, 07 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00007
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Rational Design of Dual Peptides Targeting Ghrelin and Y2 Receptors to Regulate Food Intake and Body Weight (Thu, 07 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501702q
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Identification of 2-[4-[(4-Methoxyphenyl)methoxy]-phenyl]acetonitrile and Derivatives as Potent Oct3/4 Inducers (Thu, 07 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00144
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Selenium-Containing Chrysin and Quercetin Derivatives: Attractive Scaffolds for Cancer Therapy (Thu, 07 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00230
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Design, Synthesis, and Biological Evaluation of Novel, Highly Active Soft ROCK Inhibitors (Wed, 06 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00308
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C7β-Methyl Analogues of the Orvinols: The Discovery of Kappa Opioid Antagonists with Nociceptin/Orphanin FQ Peptide (NOP) Receptor Partial Agonism and Low, or Zero, Efficacy at Mu Opioid Receptors (Wed, 06 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00130
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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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Peroxisome Proliferator-Activated Receptor γ (PPARγ) and Ligand Choreography: Newcomers Take the Stage (Thu, 09 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501155f
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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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Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis (Tue, 31 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501512b
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Clostridium difficile Drug Pipeline: Challenges in Discovery and Development of New Agents (Mon, 30 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5016846
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Fighting Malaria: Structure-Guided Discovery of Nonpeptidomimetic Plasmepsin Inhibitors (Tue, 17 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5014133
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Origins of the Quinolone Class of Antibacterials: An Expanded “Discovery Story” (Thu, 12 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501881c
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The Hippo Pathway and YAP/TAZ–TEAD Protein–Protein Interaction as Targets for Regenerative Medicine and Cancer Treatment (Wed, 11 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501615v
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A Survey of the Role of Noncovalent Sulfur Interactions in Drug Design (Tue, 03 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501853m
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Tau Positron Emission Tomography (PET) Imaging: Past, Present, and Future (Wed, 25 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5017544
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Synthetic Nucleic Acid Delivery Systems: Present and Perspectives (Fri, 20 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500330k
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Bronchodilating Drugs for Chronic Obstructive Pulmonary Disease: Current Status and Future Trends (Mon, 09 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5013227
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