Journal of Medicinal Chemistry

[ASAP] Inhibiting Hedgehog: An Update on Pharmacological Compounds and Targeting Strategies (Wed, 24 Apr 2019)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00350

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[ASAP] Correction to Synthesis of 11C-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 [11C]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)

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)

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)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00370

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[ASAP] D2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine (Thu, 18 Apr 2019)

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)

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)

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)

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)

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)

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)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01991

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[ASAP] Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain (Tue, 16 Apr 2019)

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)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b02012

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[ASAP] A2B Adenosine Receptor Antagonists with Picomolar Potency (Mon, 15 Apr 2019)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

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)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00039

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[ASAP] Correction to Remarkable Brain Penetration of Cyclopentadienyl M(CO)3+ (M = 99mTc, 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)

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)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01597

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