[ASAP] New Dual Small Molecules for Alzheimer’s Disease Therapy Combining Histamine H<sub>3</sub> Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition
(Thu, 05 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b00937
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[ASAP] Structure–Activity Relationship Studies of Pyridine-Based Ligands and Identification of a Fluorinated Derivative for Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors
(Thu, 05 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01280
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[ASAP] Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands
(Thu, 05 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01393
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[ASAP] Subtype Selective ?-Aminobutyric Acid Type A Receptor (GABA<sub>A</sub>R) Modulators Acting at the Benzodiazepine Binding Site: An Update
(Thu, 05 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01312
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[ASAP] Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5–MYC Protein–Protein Interaction
(Thu, 05 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01411
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[ASAP] 4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual µ-Opioid Receptor Agonists and s<sub>1</sub> Receptor Antagonists for the Treatment of Pain
(Thu, 05 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01256
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[ASAP] Structure-Based Optimization of Coumarin hA<sub>3</sub> Adenosine Receptor Antagonists
(Wed, 04 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01572
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[ASAP] Position Effect of Fatty Acid Modification on the Cytotoxicity and Antimetastasis Potential of the Cytotoxic Peptide Lycosin-I
(Wed, 04 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01126
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[ASAP] Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor <bold>M8891</bold>: A Clinical Compound for the Treatment of Cancer
(Tue, 03 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01070
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[ASAP] Structure-Based and Property-Driven Optimization of <italic toggle="yes">N</italic>-Aryl Imidazoles toward Potent and Selective Oral ROR?t Inhibitors
(Tue, 03 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01291
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[ASAP] Discovery of Novel Celastrol Derivatives as Hsp90–Cdc37 Interaction Disruptors with Antitumor Activity
(Tue, 03 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01290
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[ASAP] Discovery of Highly Polar ß-Homophenylalanine Derivatives as Nonsystemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors
(Tue, 03 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01649
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[ASAP] Novel Propargyl-Linked Bisubstrate Analogues as Tight-Binding Inhibitors for Nicotinamide <italic toggle="yes">N</italic>-Methyltransferase
(Tue, 03 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01255
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[ASAP] Multitarget CFTR Modulators Endowed with Multiple Beneficial Side Effects for Cystic Fibrosis Patients: Toward a Simplified Therapeutic Approach<xref rid="notes-1" ref-type="statement">†</xref>
(Tue, 03 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01416
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[ASAP] Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry
(Mon, 02 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01541
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[ASAP] Benzisothiazolinone Derivatives as Potent Allosteric Monoacylglycerol Lipase Inhibitors That Functionally Mimic Sulfenylation of Regulatory Cysteines
(Mon, 02 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01679
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[ASAP] Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells
(Mon, 02 Dec 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01405
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[ASAP] Enzymatic Preparation of 2'–5',3'–5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations
(Wed, 27 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01062
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[ASAP] Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3<italic toggle="yes">S</italic>)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7<italic toggle="yes">H</italic>-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer
(Wed, 27 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01293
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[ASAP] An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights
(Wed, 27 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01339
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[ASAP] Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis
(Wed, 27 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b00908
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[ASAP] Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader
(Wed, 27 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01528
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[ASAP] Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies
(Tue, 26 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01625
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[ASAP] Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors
(Tue, 26 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01227
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[ASAP] Correction to “Discovery and Optimization of 4,5-Diarylisoxazoles as Potent Dual Inhibitors of Pyruvate Dehydrogenase Kinase and Heat Shock Protein 90”
(Tue, 26 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01878
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[ASAP] Nonradioactive Cell Assay for the Evaluation of Modular Prostate-Specific Membrane Antigen Targeting Ligands via Inductively Coupled Plasma Mass Spectrometry
(Tue, 26 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01606
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[ASAP] Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic
(Tue, 26 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01046
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[ASAP] Rational Design and Optimization of a Novel Class of Macrocyclic Apoptosis Signal-Regulating Kinase 1 Inhibitors
(Tue, 26 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01206
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[ASAP] Optimizing Targeted Inhibitors of P-Glycoprotein Using Computational and Structure-Guided Approaches
(Tue, 26 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b00966
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[ASAP] Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation
(Mon, 25 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01194
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[ASAP] Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC)
(Mon, 25 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01295
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[ASAP] Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate
(Fri, 22 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01562
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[ASAP] Novel Brain-Tumor-Inhibiting Copper(II) Compound Based on a Human Serum Albumin (HSA)-Cell Penetrating Peptide Conjugate
(Thu, 21 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b00939
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[ASAP] The Immunoproteasome: An Emerging Target in Cancer and Autoimmune and Neurological Disorders
(Thu, 21 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01226
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[ASAP] Discovery of the First Low Nanomolar Liver Receptor Homolog-1 (LRH-1) Agonist
(Thu, 21 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01753
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[ASAP] Effect of Modifier Structure on the Activation of Leukotriene A<sub>4</sub> Hydrolase Aminopeptidase Activity
(Thu, 21 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b00663
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[ASAP] Discovery and Pharmacological Studies of 4-Hydroxyphenyl-Derived Phosphonium Salts Active in a Mouse Model of Visceral Leishmaniasis
(Thu, 21 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b00998
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[ASAP] Hit-to-Lead Optimization of Benzoxazepinoindazoles As Human African Trypanosomiasis Therapeutics
(Wed, 20 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01506
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[ASAP] 4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H<sub>3</sub> Receptor Agonists with in Vivo Central Nervous System Activity
(Wed, 20 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01462
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[ASAP] Discovery of 4<italic toggle="yes">H</italic>-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models
(Wed, 20 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01143
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[ASAP] Advances in Discovering Deubiquitinating Enzyme (DUB) Inhibitors
(Wed, 20 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01138
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[ASAP] Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug–Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis
(Fri, 15 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01130
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[ASAP] Structure–Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability
(Thu, 14 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01188
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[ASAP] Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability
(Thu, 14 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01074
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[ASAP] Structure–Activity Relationship Studies of Small Molecule Modulators of the Staphylococcal Accessory Gene Regulator
(Thu, 14 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b00798
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[ASAP] Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding
(Wed, 13 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01060
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[ASAP] ß-Lactamase Inhibitors To Restore the Efficacy of Antibiotics against Superbugs
(Wed, 13 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01279
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[ASAP] Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions
(Tue, 12 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b00940
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[ASAP] Differentiating the Pharmacodynamics and Toxicology of Macrolide and Ketolide Antibiotics<subtitle>Miniperspective</subtitle>
(Thu, 07 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01159
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[ASAP] Development and Therapeutic Potential of Selenazo Compounds
(Tue, 05 Nov 2019)
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01152
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