Journal of Medicinal Chemistry



[ASAP] Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands (Wed, 21 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00919
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[ASAP] HIV-1 Protease Inhibitors Incorporating Stereochemically Defined P2' Ligands To Optimize Hydrogen Bonding in the Substrate Envelope (Wed, 21 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00838
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[ASAP] Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents (Wed, 21 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00353
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[ASAP] Synthesis and Structure–Activity Relationship Study of Antimicrobial Auranofin against ESKAPE Pathogens (Wed, 21 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00550
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[ASAP] Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity (Tue, 20 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00656
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[ASAP] Discovery of ß-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators (Tue, 20 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00340
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[ASAP] Targeting GNE Myopathy: A Dual Prodrug Approach for the Delivery of <italic toggle="yes">N</italic>-Acetylmannosamine 6-Phosphate (Tue, 20 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00833
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[ASAP] Metabolism by Aldehyde Oxidase: Drug Design and Complementary Approaches to Challenges in Drug Discovery (Tue, 20 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00875
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[ASAP] The Development Process for Discovery and Clinical Advancement of Modern Antimalarials (Tue, 20 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00761
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[ASAP] How To Design Selective Ligands for Highly Conserved Binding Sites: A Case Study Using <italic toggle="yes">N</italic>-Myristoyltransferases as a Model System (Mon, 19 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00586
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[ASAP] Synthesis and SAR Study of Carbamoyl Pyridone Bicycle Derivatives as Potent Inhibitors of Influenza Cap-dependent Endonuclease (Mon, 19 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00861
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[ASAP] Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles (Mon, 19 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00716
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[ASAP] Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase (Mon, 19 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00687
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[ASAP] From Phenylthiazoles to Phenylpyrazoles: Broadening the Antibacterial Spectrum toward Carbapenem-Resistant Bacteria (Mon, 19 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00720
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[ASAP] Correction to Discovery of Entrectinib: A New 3-Aminoindazole as a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor (Mon, 19 Aug 2019)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01259
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[ASAP] Mucosal Vaccination with a Self-Adjuvanted Lipopeptide Is Immunogenic and Protective against <italic toggle="yes">Mycobacterium tuberculosis</italic> (Fri, 16 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00832
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[ASAP] SAR Studies on Aromatic Acylhydrazone-Based Inhibitors of Fungal Sphingolipid Synthesis as Next-Generation Antifungal Agents (Fri, 16 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b01004
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[ASAP] A New Approach in Cancer Treatment: Discovery of Chlorido[<italic toggle="yes">N</italic>,<italic toggle="yes">N</italic>'-disalicylidene-1,2-phenylenediamine]iron(III) Complexes as Ferroptosis Inducers (Thu, 15 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00814
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[ASAP] Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation (Thu, 15 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00855
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[ASAP] Developing and Characterization of Chemically Modified RNA Aptamers for Targeting Wild Type and Mutated c-KIT Receptor Tyrosine Kinases (Thu, 15 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00868
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[ASAP] Probing the Existence of a Metastable Binding Site at the ß<sub>2</sub>-Adrenergic Receptor with Homobivalent Bitopic Ligands (Thu, 15 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00595
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[ASAP] Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases (Thu, 15 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00794
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[ASAP] Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity? (Thu, 15 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00683
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[ASAP] Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor <bold>BI-4924</bold> Disrupts Serine Biosynthesis (Wed, 14 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00718
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[ASAP] Neuroactive Steroid <italic toggle="yes">N</italic>-Methyl-<sc>d</sc>-aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity (Tue, 13 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00591
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[ASAP] Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase (Fri, 09 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00625
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[ASAP] Discovery and Development of a Series of Pyrazolo[3,4-<italic toggle="yes">d</italic>]pyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design (Fri, 09 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00510
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[ASAP] A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification (Fri, 09 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00673
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[ASAP] Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis (Tue, 06 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00969
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[ASAP] Profile of a Highly Selective Quaternized Pyrrolidine Betaine a<sub>v</sub>ß<sub>6</sub> Integrin Inhibitor—(3<italic toggle="yes">S</italic>)-3-(3-(3,5-Dimethyl-1<italic toggle="yes">H</italic>-pyrazol-1-yl)phenyl)-4-((1<italic toggle="yes">S</italic> and 1<italic toggle="yes">R</italic>,3<italic toggle="yes">R</italic>)-1-methyl-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-ium-1-yl)butanoate Synthesized by Stereoselective Methylation (Mon, 05 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00819
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[ASAP] Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy (Mon, 05 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00186
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[ASAP] Cyclization of RGD Peptides by Suzuki–Miyaura Cross-Coupling (Mon, 05 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00360
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[ASAP] Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways (Fri, 02 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00030
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[ASAP] Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders (Fri, 02 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00871
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[ASAP] 2-Amino-2,3-dihydro-1<italic toggle="yes">H</italic>-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy (Fri, 02 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00365
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[ASAP] Identification of Novel Medulloblastoma Cell-Targeting Peptides for Use in Selective Chemotherapy Drug Delivery (Thu, 01 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00851
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[ASAP] Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68) (Thu, 01 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00869
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[ASAP] Precision Cancer Nanotherapy: Evolving Role of Multifunctional Nanoparticles for Cancer Active Targeting (Thu, 01 Aug 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00511
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[ASAP] Virtual Screening Approach and Investigation of Structure–Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens (Wed, 31 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00394
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[ASAP] Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1) (Wed, 24 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00522
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[ASAP] Monosaccharide Analogues of Anticancer Peptide R-Lycosin-I: Role of Monosaccharide Conjugation in Complexation and the Potential of Lung Cancer Targeting and Therapy (Thu, 18 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00634
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[ASAP] Opportunities and Challenges in Phenotypic Screening for Neurodegenerative Disease Research (Thu, 18 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00797
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[ASAP] Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165 (Thu, 18 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00444
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[ASAP] Identification of <italic toggle="yes">N</italic>-Methyl Nicotinamide and <italic toggle="yes">N</italic>-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2) (Wed, 17 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00443
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[ASAP] TASK Channels Pharmacology: New Challenges in Drug Design (Mon, 15 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00248
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[ASAP] Bio-Inspired Dual-Selective <italic toggle="yes">BCL-2</italic>/<italic toggle="yes">c-MYC</italic> G-Quadruplex Binders: Design, Synthesis, and Anticancer Activity of Drug-like Imidazo[2,1-<italic toggle="yes">i</italic>]purine Derivatives (Wed, 10 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00262
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[ASAP] In Silico Prediction of Hemolytic Toxicity on the Human Erythrocytes for Small Molecules by Machine-Learning and Genetic Algorithm (Mon, 08 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00853
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[ASAP] Norepinephrine-Transporter-Targeted and DNA-Co-Targeted Theranostic Guanidines (Wed, 03 Jul 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00437
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[ASAP] Why Some Targets Benefit from beyond Rule of Five Drugs (Wed, 26 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01732
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[ASAP] Are We Opening the Door to a New Era of Medicinal Chemistry or Being Collapsed to a Chemical Singularity?<subtitle>Perspective</subtitle> (Wed, 26 Jun 2019)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.9b00004
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