Journal of Medicinal Chemistry

[ASAP] Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective (Mon, 18 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00159
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[ASAP] Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors (Mon, 18 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00447
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[ASAP] Structural Insights of Benzenesulfonamide Analogues as NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization (Mon, 18 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00733
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[ASAP] Preferential Cleavage of a Tripeptide Linkage by Enzymes on Renal Brush Border Membrane To Reduce Renal Radioactivity Levels of Radiolabeled Antibody Fragments (Fri, 15 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00198
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[ASAP] Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson’s Disease (Fri, 15 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00204
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[ASAP] Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances (Fri, 15 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00667
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[ASAP] Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine ß-Secretase (BACE1) Inhibitors via Active Conformation Stabilization (Thu, 14 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00011
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[ASAP] Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinase ? (PI3K?) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS) (Thu, 14 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00085
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[ASAP] Computer-Assisted Discovery of Retinoid X Receptor Modulating Natural Products and Isofunctional Mimetics (Thu, 14 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00494
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[ASAP] Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity (Thu, 14 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00576
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[ASAP] Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors (Wed, 13 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00076
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[ASAP] New Modalities, Technologies, and Partnerships in Probe and Lead Generation: Enabling a Mode-of-Action Centric Paradigm (Wed, 13 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00378
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[ASAP] Development, Optimization, and Structure–Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4-<italic toggle="yes">d</italic>]pyrrolo[2,3-<italic toggle="yes">b</italic>]pyridine Scaffold (Wed, 13 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00571
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[ASAP] Discovery of ß-Adrenergic Receptors Blocker–Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy (Wed, 13 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00625
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[ASAP] Potent and Highly Selective Inhibitors of the Proteasome Trypsin-like Site by Incorporation of Basic Side Chain Containing Amino Acid Derived Sulfonyl Fluorides (Wed, 13 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00685
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[ASAP] Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis (Tue, 12 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00281
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[ASAP] Click Chemistry-Based Discovery of [3-Hydroxy-5-(1<italic toggle="yes">H</italic>-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia (Tue, 12 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00549
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[ASAP] Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine (Mon, 11 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01709
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[ASAP] Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses (Mon, 11 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00042
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[ASAP] Optimization of 1,4-Oxazine ß-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate (Mon, 11 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00304
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[ASAP] Selective Substrates and Activity-Based Probes for Imaging of the Human Constitutive 20S Proteasome in Cells and Blood Samples (Sat, 09 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00026
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[ASAP] Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds (Fri, 08 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00250
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[ASAP] Determination of Affinity and Residence Time of Potent Drug-Target Complexes by Label-free Biosensing (Thu, 07 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01829
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[ASAP] Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously (Thu, 07 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00384
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[ASAP] Emerging Approaches for the Identification of Protein Targets of Small Molecules - A Practitioners’ Perspective (Wed, 06 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01921
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[ASAP] Structure–Activity Relationships and Therapeutic Potentials of 5-HT<sub>7</sub> Receptor Ligands: An Update (Tue, 05 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01898
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[ASAP] Phosphorus-Based Probes as Molecular Tools for Proteome Studies: Recent Advances in Probe Development and Applications (Mon, 04 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00249
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[ASAP] Plasmodial Kinase Inhibitors: License to Cure? (Mon, 04 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00329
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[ASAP] Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration<subtitle>Miniperspective</subtitle> (Mon, 04 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00370
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[ASAP] Specific Stereoisomeric Conformations Determine the Drug Potency of Cladosporin Scaffold against Malarial Parasite (Mon, 04 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00565
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[ASAP] Advances and Insights for Small Molecule Inhibition of Macrophage Migration Inhibitory Factor (Mon, 04 Jun 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00589
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[ASAP] A Surprising Recipe for Designing Biased Ligands (Mon, 04 Jun 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00764
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[ASAP] Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1–Nuclear Factor Erythroid 2-Related Factor 2 (Keap1–Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases (Tue, 29 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00358
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[ASAP] Inhibitors of Melanogenesis: An Updated Review (Thu, 24 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00967
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[ASAP] Rational Design of Novel 1,3-Oxazine Based ß-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aß Reduction in the Brain (Wed, 23 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00002
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[ASAP] What Makes a Great Medicinal Chemist? A Personal Perspective<subtitle>Miniperspective</subtitle> (Tue, 22 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01445
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[ASAP] Editorial on First-Time Disclosures of Clinical Candidates (Mon, 21 May 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00739
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[ASAP] Factor XIa Inhibitors as New Anticoagulants (Fri, 18 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00173
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[ASAP] A Thieno[2,3-<italic toggle="yes">d</italic>]pyrimidine Scaffold Is a Novel Negative Allosteric Modulator of the Dopamine D<sub>2</sub> Receptor (Tue, 15 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01565
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[ASAP] Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase (Mon, 14 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01862
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[ASAP] Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example (Thu, 10 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00318
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[ASAP] Fishing for Drug Targets: A Focus on Diazirine Photoaffinity Probe Synthesis (Wed, 09 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01561
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[ASAP] Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases (Wed, 09 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01686
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[ASAP] Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over ß-Arrestin 2 Recruitment) Within the Melanocortin Receptors (Wed, 09 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00238
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[ASAP] NAD(P)H:Quinone Oxidoreductase 1 (NQO1) as a Therapeutic and Diagnostic Target in Cancer (Mon, 07 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00124
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[ASAP] Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors (Thu, 03 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00280
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[ASAP] Novel Allosteric Activators for Ferroptosis Regulator Glutathione Peroxidase 4 (Wed, 02 May 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00315
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[ASAP] Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations (Wed, 25 Apr 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00180
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[ASAP] Synthetic Approaches to New Drugs Approved During 2016 (Thu, 19 Apr 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00260
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[ASAP] Lipophilic Efficiency as an Important Metric in Drug Design (Tue, 17 Apr 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00077
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