Journal of Medicinal Chemistry



[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] Paired Utility of Aza-Amino Acyl Proline and Indolizidinone Amino Acid Residues for Peptide Mimicry: Conception of Prostaglandin F2a Receptor Allosteric Modulators That Delay Preterm Birth (Tue, 23 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00056
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[ASAP] A Selective and Brain Penetrant p38aMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction (Tue, 23 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00058
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[ASAP] Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders (Tue, 23 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00193
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[ASAP] Structure Overhaul Affords a Potent Purine PI3Kd Inhibitor with Improved Tolerability (Mon, 22 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01818
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[ASAP] Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable ROR? Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer (Mon, 22 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00327
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[ASAP] Development of Novel Epoxyketone-Based Proteasome Inhibitors as a Strategy To Overcome Cancer Resistance to Carfilzomib and Bortezomib (Fri, 19 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01943
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[ASAP] Structure-Guided Drug Design of 6-Substituted Adenosine Analogues as Potent Inhibitors of <italic toggle="yes">Mycobacterium tuberculosis</italic> Adenosine Kinase (Fri, 19 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00020
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[ASAP] Synthesis and Anti-HCV Activities of 4'-Fluoro-2'-Substituted Uridine Triphosphates and Nucleotide Prodrugs: Discovery of 4'-Fluoro-2'-<italic toggle="yes">C</italic>-methyluridine 5'-Phosphoramidate Prodrug (<bold>AL-335</bold>) for the Treatment of Hepatitis C Infection (Fri, 19 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00143
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[ASAP] Rational Design of Short Peptide Variants by Using Kunitzin-RE, an Amphibian-Derived Bioactivity Peptide, for Acquired Potent Broad-Spectrum Antimicrobial and Improved Therapeutic Potential of Commensalism Coinfection of Pathogens (Fri, 19 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00149
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[ASAP] Novel 15-Lipoxygenase-1 Inhibitor Protects Macrophages from Lipopolysaccharide-Induced Cytotoxicity (Fri, 19 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00212
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[ASAP] Discovery of [1,2,4]Triazolo[4,3-<italic toggle="yes">a</italic>]pyridines as Potent Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction (Fri, 19 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00312
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[ASAP] Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma (Fri, 19 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00350
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[ASAP] Correction to Synthesis of <sup>11</sup>C-Labeled RXR Partial Agonist 1-[(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)amino]benzotriazole-5-carboxylic Acid (CBt-PMN) by Direct [<sup>11</sup>C]Carbon Dioxide Fixation via Organolithiation of Trialkyltin Precursor and PET Imaging Thereof (Fri, 19 Apr 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00617
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[ASAP] 5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Response Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma (Thu, 18 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01772
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[ASAP] Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands (Thu, 18 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01986
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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] D<sub>2</sub> Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine (Thu, 18 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00508
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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] Identification of Three-Way DNA Junction Ligands through Screening of Chemical Libraries and Validation by Complementary in Vitro Assays (Wed, 17 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01978
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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] 3,5,7-Substituted Pyrazolo[4,3-<italic toggle="yes">d</italic>]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models (Wed, 17 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00189
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[ASAP] Correction to Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes (Wed, 17 Apr 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00559
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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] Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer (Tue, 16 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01991
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[ASAP] Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na<sub>v</sub>1.7 Inhibitors for the Treatment of Chronic Pain (Tue, 16 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00141
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[ASAP] Novel Chemical Series of 5-Lipoxygenase-Activating Protein Inhibitors for Treatment of Coronary Artery Disease (Mon, 15 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b02012
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[ASAP] A<sub>2B</sub> Adenosine Receptor Antagonists with Picomolar Potency (Mon, 15 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00071
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[ASAP] Novel Lysine-Based Thioureas as Mechanism-Based Inhibitors of Sirtuin 2 (SIRT2) with Anticancer Activity in a Colorectal Cancer Murine Model (Mon, 15 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00191
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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] Identification of Pyrrolo[2,3-<italic toggle="yes">d</italic>]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia (Mon, 15 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00223
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[ASAP] Design and Synthesis of Type-IV Inhibitors of BRAF Kinase That Block Dimerization and Overcome Paradoxical MEK/ERK Activation (Fri, 12 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01288
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[ASAP] Fragment-Based Discovery of a Qualified Hit Targeting the Latency-Associated Nuclear Antigen of the Oncogenic Kaposi’s Sarcoma-Associated Herpesvirus/Human Herpesvirus 8 (Fri, 12 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01827
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[ASAP] Discovery, Optimization, and Target Identification of Novel Potent Broad-Spectrum Antiviral Inhibitors (Fri, 12 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00091
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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] Fragment-Based Discovery of an Apolipoprotein E4 (apoE4) Stabilizer (Fri, 12 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00178
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[ASAP] Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic µ-Opioid Receptor (MOR) Agonist/d-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability (Fri, 12 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00219
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[ASAP] Synthesis and Structure–Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety (Fri, 12 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00449
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[ASAP] Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants (Wed, 10 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01845
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[ASAP] Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma (Wed, 10 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00282
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[ASAP] Galloyl Carbohydrates with Antiangiogenic Activity Mediated by Capillary Morphogenesis Gene 2 (CMG2) Protein Binding (Tue, 09 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01988
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[ASAP] Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections (Tue, 09 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b02021
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[ASAP] Dual Pharmacophores Explored via Structure–Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design (Tue, 09 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00378
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[ASAP] Anti-Zika Activity of a Library of Synthetic Carbohydrate Receptors (Mon, 08 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00142
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[ASAP] Structure–Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors (Fri, 05 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01283
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[ASAP] Novel Pyrazolo[4,3-<italic toggle="yes">d</italic>]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model (Fri, 05 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00039
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[ASAP] Correction to Remarkable Brain Penetration of Cyclopentadienyl M(CO)<sub>3</sub><sup>+</sup> (M = <sup>99m</sup>Tc, Re) Derivatives of Benzothiazole and Benzimidazole Paves the Way for Their Application as Diagnostic, with Single-Photon-Emission Computed Tomography (SPECT), and Therapeutic Agents for Alzheimer’s Disease (Fri, 05 Apr 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00529
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[ASAP] Women in Medicinal Chemistry Special Issue Call for Papers (Fri, 05 Apr 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00534
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[ASAP] Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia (Wed, 03 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01041
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[ASAP] Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies (Wed, 03 Apr 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01597
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