Journal of Medicinal Chemistry



[ASAP] New Dual Small Molecules for Alzheimer’s Disease Therapy Combining Histamine H<sub>3</sub> Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition (Thu, 05 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00937
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[ASAP] Structure–Activity Relationship Studies of Pyridine-Based Ligands and Identification of a Fluorinated Derivative for Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors (Thu, 05 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01280
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[ASAP] Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands (Thu, 05 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01393
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[ASAP] Subtype Selective ?-Aminobutyric Acid Type A Receptor (GABA<sub>A</sub>R) Modulators Acting at the Benzodiazepine Binding Site: An Update (Thu, 05 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01312
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[ASAP] Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5–MYC Protein–Protein Interaction (Thu, 05 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01411
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[ASAP] 4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual µ-Opioid Receptor Agonists and s<sub>1</sub> Receptor Antagonists for the Treatment of Pain (Thu, 05 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01256
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[ASAP] Structure-Based Optimization of Coumarin hA<sub>3</sub> Adenosine Receptor Antagonists (Wed, 04 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01572
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[ASAP] Position Effect of Fatty Acid Modification on the Cytotoxicity and Antimetastasis Potential of the Cytotoxic Peptide Lycosin-I (Wed, 04 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01126
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[ASAP] Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor <bold>M8891</bold>: A Clinical Compound for the Treatment of Cancer (Tue, 03 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01070
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[ASAP] Structure-Based and Property-Driven Optimization of <italic toggle="yes">N</italic>-Aryl Imidazoles toward Potent and Selective Oral ROR?t Inhibitors (Tue, 03 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01291
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[ASAP] Discovery of Novel Celastrol Derivatives as Hsp90–Cdc37 Interaction Disruptors with Antitumor Activity (Tue, 03 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01290
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[ASAP] Discovery of Highly Polar ß-Homophenylalanine Derivatives as Nonsystemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors (Tue, 03 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01649
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[ASAP] Novel Propargyl-Linked Bisubstrate Analogues as Tight-Binding Inhibitors for Nicotinamide <italic toggle="yes">N</italic>-Methyltransferase (Tue, 03 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01255
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[ASAP] Multitarget CFTR Modulators Endowed with Multiple Beneficial Side Effects for Cystic Fibrosis Patients: Toward a Simplified Therapeutic Approach<xref rid="notes-1" ref-type="statement">†</xref> (Tue, 03 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01416
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[ASAP] Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry (Mon, 02 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01541
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[ASAP] Benzisothiazolinone Derivatives as Potent Allosteric Monoacylglycerol Lipase Inhibitors That Functionally Mimic Sulfenylation of Regulatory Cysteines (Mon, 02 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01679
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[ASAP] Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells (Mon, 02 Dec 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01405
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[ASAP] Enzymatic Preparation of 2'–5',3'–5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations (Wed, 27 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01062
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[ASAP] Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3<italic toggle="yes">S</italic>)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7<italic toggle="yes">H</italic>-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer (Wed, 27 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01293
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[ASAP] An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights (Wed, 27 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01339
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[ASAP] Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis (Wed, 27 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00908
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[ASAP] Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader (Wed, 27 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01528
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[ASAP] Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies (Tue, 26 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01625
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[ASAP] Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors (Tue, 26 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01227
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[ASAP] Correction to “Discovery and Optimization of 4,5-Diarylisoxazoles as Potent Dual Inhibitors of Pyruvate Dehydrogenase Kinase and Heat Shock Protein 90” (Tue, 26 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01878
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[ASAP] Nonradioactive Cell Assay for the Evaluation of Modular Prostate-Specific Membrane Antigen Targeting Ligands via Inductively Coupled Plasma Mass Spectrometry (Tue, 26 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01606
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[ASAP] Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic (Tue, 26 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01046
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[ASAP] Rational Design and Optimization of a Novel Class of Macrocyclic Apoptosis Signal-Regulating Kinase 1 Inhibitors (Tue, 26 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01206
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[ASAP] Optimizing Targeted Inhibitors of P-Glycoprotein Using Computational and Structure-Guided Approaches (Tue, 26 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00966
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[ASAP] Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation (Mon, 25 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01194
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[ASAP] Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC) (Mon, 25 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01295
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[ASAP] Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate (Fri, 22 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01562
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[ASAP] Novel Brain-Tumor-Inhibiting Copper(II) Compound Based on a Human Serum Albumin (HSA)-Cell Penetrating Peptide Conjugate (Thu, 21 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00939
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[ASAP] The Immunoproteasome: An Emerging Target in Cancer and Autoimmune and Neurological Disorders (Thu, 21 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01226
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[ASAP] Discovery of the First Low Nanomolar Liver Receptor Homolog-1 (LRH-1) Agonist (Thu, 21 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01753
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[ASAP] Effect of Modifier Structure on the Activation of Leukotriene A<sub>4</sub> Hydrolase Aminopeptidase Activity (Thu, 21 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00663
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[ASAP] Discovery and Pharmacological Studies of 4-Hydroxyphenyl-Derived Phosphonium Salts Active in a Mouse Model of Visceral Leishmaniasis (Thu, 21 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00998
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[ASAP] Hit-to-Lead Optimization of Benzoxazepinoindazoles As Human African Trypanosomiasis Therapeutics (Wed, 20 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01506
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[ASAP] 4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H<sub>3</sub> Receptor Agonists with in Vivo Central Nervous System Activity (Wed, 20 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01462
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[ASAP] Discovery of 4<italic toggle="yes">H</italic>-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models (Wed, 20 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01143
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[ASAP] Advances in Discovering Deubiquitinating Enzyme (DUB) Inhibitors (Wed, 20 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01138
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[ASAP] Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug–Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis (Fri, 15 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01130
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[ASAP] Structure–Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability (Thu, 14 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01188
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[ASAP] Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability (Thu, 14 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01074
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[ASAP] Structure–Activity Relationship Studies of Small Molecule Modulators of the Staphylococcal Accessory Gene Regulator (Thu, 14 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00798
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[ASAP] Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding (Wed, 13 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01060
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[ASAP] ß-Lactamase Inhibitors To Restore the Efficacy of Antibiotics against Superbugs (Wed, 13 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01279
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[ASAP] Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions (Tue, 12 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00940
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[ASAP] Differentiating the Pharmacodynamics and Toxicology of Macrolide and Ketolide Antibiotics<subtitle>Miniperspective</subtitle> (Thu, 07 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01159
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[ASAP] Development and Therapeutic Potential of Selenazo Compounds (Tue, 05 Nov 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01152
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