Journal of Medicinal Chemistry



[ASAP] Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A<sub>3</sub> Adenosine Receptors: Affinity Enhancement by <italic toggle="yes">N</italic><sup>6</sup>-(2-Phenylethyl) Substitution (Thu, 09 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00235
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[ASAP] Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity (Thu, 09 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00211
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[ASAP] Emerging Substrate Proteins of Kelch-like ECH Associated Protein 1 (Keap1) and Potential Challenges for the Development of Small-Molecule Inhibitors of the Keap1-Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Protein–Protein Interaction (Wed, 08 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01865
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[ASAP] Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors (Wed, 08 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00193
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[ASAP] Discovery of Potent and Selective Non-Nucleotide Small Molecule Inhibitors of CD73 (Wed, 08 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01713
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[ASAP] Novel Stapling by Lysine Tethering Provides Stable and Low Hemolytic Cationic Antimicrobial Peptides (Wed, 08 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02025
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[ASAP] Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability (Wed, 08 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01658
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[ASAP] Discovery of 8-Methyl-pyrrolo[1,2-<italic toggle="yes">a</italic>]pyrazin-1(2<italic toggle="yes">H</italic>)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors (Tue, 07 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01784
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[ASAP] Modulating Heparanase Activity: Tuning Sulfation Pattern and Glycosidic Linkage of Oligosaccharides (Tue, 07 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00156
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[ASAP] Discovery of a Potent and Selective NF-?B-Inducing Kinase (NIK) Inhibitor That Has Anti-inflammatory Effects in Vitro and in Vivo (Tue, 07 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00396
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[ASAP] GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage (Tue, 07 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02176
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[ASAP] Identification of the Clinical Development Candidate <bold>MRTX849</bold>, a Covalent KRAS<sup>G12C</sup> Inhibitor for the Treatment of Cancer (Mon, 06 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02052
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[ASAP] Design, Synthesis, and Conformation–Activity Study of Unnatural Bridged Bicyclic Depsipeptides as Highly Potent Hypoxia Inducible Factor-1 Inhibitors and Antitumor Agents (Thu, 02 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02039
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[ASAP] Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads (Thu, 02 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02129
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[ASAP] CN128: A New Orally Active Hydroxypyridinone Iron Chelator (Thu, 02 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00137
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[ASAP] Thiazoles, Their Benzofused Systems, and Thiazolidinone Derivatives: Versatile and Promising Tools to Combat Antibiotic Resistance (Thu, 02 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01245
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[ASAP] Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases (Thu, 02 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01451
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[ASAP] Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-ß-lactamases (Thu, 02 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01976
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[ASAP] Machine Learning in Mass Spectrometry: A MALDI-TOF MS Approach to Phenotypic Antibacterial Screening (Wed, 01 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00040
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[ASAP] Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer (Wed, 01 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00045
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[ASAP] Structurally Strained Half-Sandwich Iridium(III) Complexes As Highly Potent Anticancer Agents (Wed, 01 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02000
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[ASAP] 2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment (Wed, 01 Apr 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01765
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[ASAP] Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model (Tue, 31 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01895
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[ASAP] An Artificial Intelligence Approach to Proactively Inspire Drug Discovery with Recommendations (Mon, 30 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02130
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[ASAP] Validation and Characterization of Five Distinct Novel Inhibitors of Human Cytomegalovirus (Fri, 27 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01501
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[ASAP] <italic toggle="yes">N</italic>-Acylethanolamine Acid Amidase (NAAA): Structure, Function, and Inhibition (Thu, 26 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.0c00191
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[ASAP] How We Think about Targeting RNA with Small Molecules (Thu, 26 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01927
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[ASAP] Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine’s Biological Activity (Mon, 23 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01924
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[ASAP] Automated De Novo Design in Medicinal Chemistry: Which Types of Chemistry Does a Generative Neural Network Learn? (Fri, 20 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02044
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[ASAP] CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? (Thu, 19 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01985
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[ASAP] Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma (Thu, 19 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01928
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[ASAP] Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown (Thu, 19 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02058
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[ASAP] Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents (Thu, 19 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b02071
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[ASAP] Metabolic and Pharmaceutical Aspects of Fluorinated Compounds (Tue, 17 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01877
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[ASAP] A Physiologically Based <italic toggle="yes">in Silico</italic> Tool to Assess the Risk of Drug-Related Crystalluria (Fri, 13 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01995
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[ASAP] Substituent Position of Iminocyclitols Determines the Potency and Selectivity for Gut Microbial Xenobiotic-Reactivating Enzymes (Mon, 09 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01918
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[ASAP] Effective Application of Metabolite Profiling in Drug Design and Discovery (Fri, 06 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01840
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[ASAP] Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types (Thu, 05 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01896
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[ASAP] Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase (Wed, 04 Mar 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01916
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[ASAP] Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death (Thu, 27 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01990
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[ASAP] a-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment (Mon, 24 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01828
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[ASAP] Cutaneous Adverse Events Caused by Sulfonamide-Containing Drugs: Reality or Perception? (Mon, 24 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01932
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[ASAP] The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology (Fri, 21 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01956
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[ASAP] Understanding Idiosyncratic Toxicity: Lessons Learned from Drug-Induced Liver Injury (Fri, 21 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01297
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[ASAP] Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success (Thu, 20 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01810
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[ASAP] DNA-Encoded Library Screening as Core Platform Technology in Drug Discovery: Its Synthetic Method Development and Applications in DEL Synthesis (Wed, 19 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01782
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[ASAP] Discovery of 4-((2<italic toggle="yes">S</italic>,4<italic toggle="yes">S</italic>)-4-Ethoxy-1-((5-methoxy-7-methyl-1<italic toggle="yes">H</italic>-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases (Wed, 19 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01870
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[ASAP] Acetylene Group, Friend or Foe in Medicinal Chemistry (Wed, 19 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01617
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[ASAP] Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (Mon, 17 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01743
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[ASAP] Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs)<subtitle>Miniperspective</subtitle> (Mon, 17 Feb 2020)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01738
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