Journal of Medicinal Chemistry

[ASAP] Evaluation of Novel Tumor-Targeted Near-Infrared Probe for Fluorescence-Guided Surgery of Cancer (Fri, 19 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01115

>> Read More

[ASAP] Optimization of 8-Hydroxyquinolines as Inhibitors of Catechol <italic toggle="yes">O</italic>-Methyltransferase (Fri, 19 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01126

>> Read More

[ASAP] Discovery of a Branched Peptide That Recognizes the Rev Response Element (RRE) RNA and Blocks HIV-1 Replication (Thu, 18 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01076

>> Read More

[ASAP] Design and Activity of Specific Hypoxia-Inducible Factor-2a (HIF-2a) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (<italic toggle="yes">S</italic>)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1<italic toggle="yes">H</italic>-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385) (Thu, 18 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01196

>> Read More

[ASAP] Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4) (Thu, 18 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01317

>> Read More

[ASAP] [99mTc][Tc(N)PNP43]-Labeled RGD Peptides As New Probes for a Selective Detection of avß3 Integrin: Synthesis, Structure–Activity and Pharmacokinetic Studies (Wed, 17 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01075

>> Read More

[ASAP] Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists (Wed, 17 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01077

>> Read More

[ASAP] Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action (Wed, 17 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01245

>> Read More

[ASAP] Clearance in Drug Design<subtitle>Miniperspective</subtitle> (Wed, 17 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01263

>> Read More

[ASAP] Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor (Tue, 16 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01248

>> Read More

[ASAP] Synthesis and Cytotoxic and Antiviral Profiling of Pyrrolo- and Furo-Fused 7-Deazapurine Ribonucleosides (Tue, 16 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01258

>> Read More

[ASAP] Alkyl Sulfinates: Radical Precursors Enabling Drug Discovery<subtitle>Miniperspective</subtitle> (Tue, 16 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01303

>> Read More

[ASAP] Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose–Response Curves against Multidrug Resistant Parasite Strains (Tue, 16 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01333

>> Read More

[ASAP] Correction to Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-Negative Bacteria (Tue, 16 Oct 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01538

>> Read More

[ASAP] Rational Design, Synthesis, and Pharmacological Characterization of Novel Ghrelin Receptor Inverse Agonists as Potential Treatment against Obesity-Related Metabolic Diseases (Mon, 15 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00794

>> Read More

[ASAP] Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine) (Fri, 12 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00141

>> Read More

[ASAP] Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors (Fri, 12 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00819

>> Read More

[ASAP] Discovery of a Potent Thiazolidine Free Fatty Acid Receptor 2 Agonist with Favorable Pharmacokinetic Properties (Fri, 12 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00855

>> Read More

[ASAP] Correction to Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors (Fri, 12 Oct 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01414

>> Read More

[ASAP] Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2 (Thu, 11 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00605

>> Read More

[ASAP] Alkyl-guanidine Compounds as Potent Broad-Spectrum Antibacterial Agents: Chemical Library Extension and Biological Characterization (Thu, 11 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00619

>> Read More

[ASAP] Design of a True Bivalent Ligand with Picomolar Binding Affinity for a G Protein-Coupled Receptor Homodimer (Thu, 11 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01249

>> Read More

[ASAP] Activity-Based Protein Profiling Delivers Selective Drug Candidate ABX-1431, a Monoacylglycerol Lipase Inhibitor, To Control Lipid Metabolism in Neurological Disorders (Thu, 11 Oct 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01405

>> Read More

[ASAP] Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents (Wed, 10 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00559

>> Read More

[ASAP] Design, Synthesis, and Evaluation of Piperazinyl Pyrrolidin-2-ones as a Novel Series of Reversible Monoacylglycerol Lipase Inhibitors (Wed, 10 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00824

>> Read More

[ASAP] Discovery, Structure–Activity Relationship, and Biological Characterization of a Novel Series of 6-((1<italic toggle="yes">H</italic>-Pyrazolo[4,3-<italic toggle="yes">b</italic>]pyridin-3-yl)amino)-benzo[<italic toggle="yes">d</italic>]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4) (Wed, 10 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00994

>> Read More

[ASAP] Single Amino Acid Substitution in a-Conotoxin TxID Reveals a Specific a3ß4 Nicotinic Acetylcholine Receptor Antagonist (Tue, 09 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00967

>> Read More

[ASAP] Novel Hypoxia-Inducible Factor 1a (HIF-1a) Inhibitors for Angiogenesis-Related Ocular Diseases: Discovery of a Novel Scaffold via Ring-Truncation Strategy (Tue, 09 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00971

>> Read More

[ASAP] Development of Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Signaling Pathway (Tue, 09 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00990

>> Read More

[ASAP] Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives (Mon, 08 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01137

>> Read More

[ASAP] How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? (Fri, 05 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00049

>> Read More

[ASAP] <italic toggle="yes">In Vivo</italic> Selectivity and Localization of Reactive Oxygen Species (ROS) Induction by Osmium Anticancer Complexes That Circumvent Platinum Resistance (Fri, 05 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00958

>> Read More

[ASAP] GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like (Fri, 05 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01225

>> Read More

[ASAP] Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter (Thu, 04 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00542

>> Read More

[ASAP] Targeting Cytochrome P450 (CYP) 1B1 Enzyme with Four Series of A-Ring Substituted Estrane Derivatives: Design, Synthesis, Inhibitory Activity, and Selectivity (Wed, 03 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00907

>> Read More

[ASAP] Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against <italic toggle="yes">Trypanosoma cruzi</italic> (Wed, 03 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00999

>> Read More

[ASAP] Application of Virtual Screening to the Identification of New LpxC Inhibitor Chemotypes, Oxazolidinone and Isoxazoline (Wed, 03 Oct 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01287

>> Read More

[ASAP] Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs<subtitle>Miniperspective</subtitle> (Thu, 27 Sep 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00686

>> Read More

[ASAP] Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application (Wed, 19 Sep 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01092

>> Read More

[ASAP] Allosteric Activation of Striatal-Enriched Protein Tyrosine Phosphatase (STEP, PTPN5) by a Fragment-like Molecule (Wed, 12 Sep 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00857

>> Read More

[ASAP] Virtual Chemical Libraries<subtitle>Miniperspective</subtitle> (Mon, 10 Sep 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01048

>> Read More

[ASAP] Discovery of 3-Cyano-<italic toggle="yes">N</italic>-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1<italic toggle="yes">H</italic>-pyrrolo[2,3-<italic toggle="yes">b</italic>]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist (Sun, 09 Sep 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00392

>> Read More

[ASAP] Overview of the Development of Glutaminase Inhibitors: Achievements and Future Directions (Fri, 07 Sep 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00961

>> Read More

[ASAP] Cubanes in Medicinal Chemistry (Thu, 06 Sep 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00888

>> Read More

[ASAP] Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts (Tue, 28 Aug 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00875

>> Read More

[ASAP] Positron Emission Tomography (PET) Ligand Development for Ionotropic Glutamate Receptors: Challenges and Opportunities for Radiotracer Targeting <italic toggle="yes">N</italic>-Methyl-<sc>d</sc>-aspartate (NMDA), a-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA), and Kainate Receptors<subtitle>Miniperspective</subtitle> (Mon, 27 Aug 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00714

>> Read More

[ASAP] Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders (Thu, 23 Aug 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00951

>> Read More

[ASAP] Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle (Wed, 22 Aug 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00802

>> Read More

[ASAP] Thermodynamics of DNA Minor Groove Binders<subtitle>Perspective</subtitle> (Tue, 14 Aug 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00233

>> Read More

[ASAP] Allosteric Modulators of HSP90 and HSP70: Dynamics Meets Function through Structure-Based Drug Design (Thu, 09 Aug 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00825

>> Read More