Journal of Medicinal Chemistry



[ASAP] Discovery of AM-6494: A Potent and Orally Efficacious ß-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2 (Fri, 18 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01034
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[ASAP] Theranostic Gallium Siderophore Ciprofloxacin Conjugate with Broad Spectrum Antibiotic Potency (Thu, 17 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01388
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[ASAP] SAR Exploration of Tight-Binding Inhibitors of Influenza Virus PA Endonuclease (Thu, 17 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00747
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[ASAP] Colocalization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor (Thu, 17 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00283
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[ASAP] Protein Stability Effects in Aggregate-Based Enzyme Inhibition (Thu, 17 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01019
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[ASAP] Chirality-Driven Mode of Binding of a-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS) (Wed, 16 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01104
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[ASAP] Metallacarborane Sulfamides: Unconventional, Specific, and Highly Selective Inhibitors of Carbonic Anhydrase IX (Wed, 16 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00945
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[ASAP] Hot-Spots of Mcl-1 Protein<subtitle>Miniperspective</subtitle> (Wed, 16 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00983
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[ASAP] Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors (Wed, 16 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00835
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[ASAP] Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3 (Wed, 16 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01283
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[ASAP] Correction to “Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges” (Wed, 16 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01619
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[ASAP] Extracellular vs Intracellular Delivery of CO: Does It Matter for a Stable, Diffusible Gasotransmitter? (Wed, 16 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01254
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[ASAP] Selective Phenylimidazole-Based Inhibitors of the <italic toggle="yes">Mycobacterium tuberculosis</italic> Proteasome (Tue, 15 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01187
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[ASAP] Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine D<sub>3</sub> Receptor Antagonists and Partial Agonists (Tue, 15 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00607
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[ASAP] A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function (Tue, 15 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00562
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[ASAP] Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases (Mon, 14 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00533
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[ASAP] Dual-Acting Cholinesterase–Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo (Mon, 14 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00623
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[ASAP] Highly Selective Butyrylcholinesterase Inhibitors with Tunable Duration of Action by Chemical Modification of Transferable Carbamate Units Exhibit Pronounced Neuroprotective Effect in an Alzheimer’s Disease Mouse Model (Mon, 14 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01012
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[ASAP] Development of Chemical Entities Endowed with Potent Fast-Killing Properties against <italic toggle="yes">Plasmodium falciparum</italic> Malaria Parasites (Mon, 14 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01099
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[ASAP] Cyanine–Gemcitabine Conjugates as Targeted Theranostic Agents for Glioblastoma Tumor Cells (Fri, 11 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01147
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[ASAP] Anti-biofilm Agents against <italic toggle="yes">Pseudomonas aeruginosa</italic>: A Structure–Activity Relationship Study of <italic toggle="yes">C</italic>-Glycosidic LecB Inhibitors (Fri, 11 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01120
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[ASAP] Tyrosine Kinase 2 (TYK2) Allosteric Inhibitors To Treat Autoimmune Diseases (Fri, 11 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01612
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[ASAP] Correction to A Novel Covalent mTOR Inhibitor, DHM25, Shows in Vivo Antitumor Activity against Triple-Negative Breast Cancer Cells (Fri, 11 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01578
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[ASAP] p97: An Emerging Target for Cancer, Neurodegenerative Diseases, and Viral Infections (Wed, 09 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01318
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[ASAP] Homodimeric Tobramycin Adjuvant Repurposes Novobiocin as an Effective Antibacterial Agent against Gram-Negative Bacteria (Wed, 09 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00876
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[ASAP] Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4) (Wed, 09 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01247
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[ASAP] The Exploration of Chirality for Improved Druggability within the Human Kinome (Wed, 09 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00640
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[ASAP] Discovery of an Extremely Potent Thiazine-Based ß-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose (Tue, 08 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01140
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[ASAP] Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy (Tue, 08 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01108
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[ASAP] Identification of 2,6-Disubstituted 3<italic toggle="yes">H</italic>-Imidazo[4,5-<italic toggle="yes">b</italic>]pyridines as Therapeutic Agents for Dysferlinopathies through Phenotypic Screening on Patient-Derived Induced Pluripotent Stem Cells (Mon, 07 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01100
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[ASAP] Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis (Mon, 07 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01025
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[ASAP] Trifluorinated Pyrimidine-Based A<sub>2B</sub> Antagonists: Optimization and Evidence of Stereospecific Recognition (Fri, 04 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01340
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[ASAP] Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and <italic toggle="yes">Trypanosoma cruzi</italic> Cruzain (Fri, 04 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00294
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[ASAP] Drugs for the Treatment of Zika Virus Infection (Fri, 04 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00775
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[ASAP] Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1a Signaling Inhibitors with Potent Activities of Anticancer Metastasis (Fri, 04 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01313
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[ASAP] <italic toggle="yes">N</italic>-Benzyl/Aryl Substituted Tryptanthrin as Dual Inhibitors of Indoleamine 2,3-Dioxygenase and Tryptophan 2,3-Dioxygenase (Thu, 03 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01079
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[ASAP] Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na<sub>V</sub>1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy (Thu, 03 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01032
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[ASAP] Correction to Mahanine, A DNA Minor Groove Binding Agent Exerts Cellular Cytotoxicity with Involvement of C-7-OH and -NH Functional Groups (Thu, 03 Oct 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01539
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[ASAP] Development of an ENPP1 Fluorescence Probe for Inhibitor Screening, Cellular Imaging, and Prognostic Assessment of Malignant Breast Cancer (Thu, 03 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01213
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[ASAP] Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel–Lindau (VHL) E3 Ubiquitin Ligase (Wed, 02 Oct 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01264
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[ASAP] Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies (Sun, 29 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01090
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[ASAP] Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease (Fri, 27 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00584
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[ASAP] The Rise of Molecules Able To Regenerate the Central Nervous System (Fri, 27 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00863
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[ASAP] Targeting of Fumarate Hydratase from <italic toggle="yes">Mycobacterium tuberculosis</italic> Using Allosteric Inhibitors with a Dimeric-Binding Mode (Fri, 27 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01203
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[ASAP] Interpretation of Compound Activity Predictions from Complex Machine Learning Models Using Local Approximations and Shapley Values (Thu, 26 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01101
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[ASAP] Design and Synthesis of Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors (Thu, 26 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00826
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[ASAP] Inhibition of the Cytolytic Protein Perforin Prevents Rejection of Transplanted Bone Marrow Stem Cells in Vivo (Thu, 26 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00881
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[ASAP] Practical High-Quality Electrostatic Potential Surfaces for Drug Discovery Using a Graph-Convolutional Deep Neural Network (Wed, 25 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01129
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[ASAP] 2016 Philip S. Portoghese Medicinal Chemistry Lectureship: Designing Bivalent or Bitopic Molecules for G-Protein Coupled Receptors. The Whole Is Greater Than the Sum of Its Parts (Tue, 24 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01105
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[ASAP] Progress in Conductive Polyaniline-Based Nanocomposites for Biomedical Applications: A Review (Tue, 24 Sep 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00803
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