Journal of Medicinal Chemistry



[ASAP] Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein–Protein Interaction (Sat, 22 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00021
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[ASAP] Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor (Sat, 22 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00727
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[ASAP] Design, Synthesis, and Efficacy Testing of Nitroethylene- and 7-Nitrobenzoxadiazol-Based Flavodoxin Inhibitors against <italic toggle="yes">Helicobacter pylori</italic> Drug-Resistant Clinical Strains and in <italic toggle="yes">Helicobacter pylori</italic>-Infected Mice (Fri, 21 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00355
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[ASAP] Linker Optimization and Therapeutic Evaluation of Phosphatidylserine-Targeting Zinc Dipicolylamine-based Drug Conjugates (Thu, 20 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00173
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[ASAP] Design, Synthesis, and Anti-RNA Virus Activity of 6'-Fluorinated-Aristeromycin Analogues (Thu, 20 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00781
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[ASAP] Improvement of Asparagine Ethylenediamines as Anti-malarial <italic toggle="yes">Plasmodium</italic>-Selective Proteasome Inhibitors (Thu, 20 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00363
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[ASAP] (<italic toggle="yes">S</italic>)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase (Thu, 20 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00525
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[ASAP] Correction to “Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors” (Wed, 19 Jun 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00852
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[ASAP] A Potent Isoprenylcysteine Carboxylmethyltransferase (ICMT) Inhibitor Improves Survival in Ras-Driven Acute Myeloid Leukemia (Wed, 19 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00145
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[ASAP] Design, Synthesis, and Structure–Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-a Motif Kinase (ZAK) Inhibitors (Mon, 17 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00664
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[ASAP] Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors (Mon, 17 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00631
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[ASAP] Synthesis and Structure–Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3-<italic toggle="yes">b</italic>]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity (Wed, 12 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00136
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[ASAP] Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the “Selectivity Pocket”, Substrate-Binding Site, and NAD<sup>+</sup>-Binding Site (Wed, 12 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00255
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[ASAP] Correction to Antimicrobial Peptides with High Proteolytic Resistance for Combating Gram-Negative Bacteria (Wed, 12 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00877
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[ASAP] Correction to “Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine” (Wed, 12 Jun 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00844
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[ASAP] Identifying Novel Anti-Osteoporosis Leads with a Chemotype-Assembly Approach (Fri, 07 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00517
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[ASAP] Five-Membered <italic toggle="yes">N</italic>-Heterocyclic Scaffolds as Novel Amino Bioisosteres at ?-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters (Wed, 05 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00026
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[ASAP] Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index (Tue, 04 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00171
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[ASAP] Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases (Wed, 29 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00390
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[ASAP] Halogens in Protein–Ligand Binding Mechanism: A Structural Perspective (Tue, 28 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01453
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[ASAP] Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms (Tue, 28 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00017
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[ASAP] <italic toggle="yes">N</italic>-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[<italic toggle="yes">d</italic>]thiazol-2-yl)cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure–Activity Relationships, and in Vivo Efficacy (Tue, 28 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00611
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[ASAP] Hydroxyl Groups in Synthetic and Natural-Product-Derived Therapeutics: A Perspective on a Common Functional Group (Tue, 28 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00179
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[ASAP] Overview of Recent Strategic Advances in Medicinal Chemistry (Tue, 28 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00359
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[ASAP] Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors (Fri, 24 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00439
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[ASAP] Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure–Activity Relationships (Thu, 23 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00335
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[ASAP] Exploiting Structural Dynamics To Design Open-Flap Inhibitors of Malarial Aspartic Proteases (Thu, 16 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00184
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[ASAP] Antibiotic Adjuvants: Make Antibiotics Great Again! (Thu, 16 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01781
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[ASAP] Design and Discovery of <italic toggle="yes">N</italic>-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic (Thu, 16 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00161
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[ASAP] Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics<subtitle>Miniperspective</subtitle> (Thu, 09 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01891
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[ASAP] Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na<sub>V</sub>1.7 (Tue, 07 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01906
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[ASAP] Pharmacological Chaperones for the Treatment of a-Mannosidosis (Thu, 02 May 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00153
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[ASAP] Fixing the Unfixable: The Art of Optimizing Natural Products for Human Medicine (Fri, 26 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00246
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[ASAP] Design and Identification of a Novel, Functionally Subtype Selective GABA<sub>A</sub> Positive Allosteric Modulator (PF-06372865) (Fri, 26 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00322
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[ASAP] Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues (Thu, 25 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00182
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[ASAP] Inhibiting Hedgehog: An Update on Pharmacological Compounds and Targeting Strategies (Wed, 24 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00188
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[ASAP] Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance (Thu, 18 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00370
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[ASAP] Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases<subtitle>Miniperspective</subtitle> (Wed, 17 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01954
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[ASAP] Recent Advances in the Exploration of Therapeutic Analogues of Gramicidin S, an Old but Still Potent Antimicrobial Peptide (Wed, 17 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00156
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[ASAP] Targeting the Thioredoxin System as a Strategy for Cancer Therapy<subtitle>Miniperspective</subtitle> (Tue, 16 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01595
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[ASAP] Synthetic Approaches to the New Drugs Approved During 2017 (Mon, 15 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00196
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[ASAP] Fifty Years in Search of Selective Antiviral Drugs<subtitle>Miniperspective</subtitle> (Fri, 12 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00175
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[ASAP] Vitamin D and Its Synthetic Analogs (Tue, 02 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00208
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[ASAP] Deciphering the Rules of in Silico Autophagy Methods for Expediting Medicinal Research<subtitle>Miniperspective</subtitle> (Thu, 28 Mar 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01673
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[ASAP] Structure-Based Macrocycle Design in Small-Molecule Drug Discovery and Simple Metrics To Identify Opportunities for Macrocyclization of Small-Molecule Ligands (Fri, 22 Mar 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01985
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[ASAP] Proteasome Activation as a New Therapeutic Approach To Target Proteotoxic Disorders (Thu, 14 Mar 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00101
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[ASAP] Emerging Trends in Flow Chemistry and Applications to the Pharmaceutical Industry (Fri, 08 Mar 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01760
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[ASAP] Allosteric Modulator Discovery: From Serendipity to Structure-Based Design (Thu, 07 Mar 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01749
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[ASAP] Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases (Fri, 01 Mar 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01651
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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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