Journal of Medicinal Chemistry

Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity (Wed, 26 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00597
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Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors (Tue, 25 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00360
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Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension (Tue, 25 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00523
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Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists (Tue, 25 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00091
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Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity (Tue, 25 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00671
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Simultaneous Drug Targeting of the Promoter MYC G-Quadruplex and BCL2 i-Motif in Diffuse Large B-Cell Lymphoma Delays Tumor Growth (Tue, 25 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00298
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Discovery of a Membrane-Active, Ring-Modified Histidine Containing Ultrashort Amphiphilic Peptide That Exhibits Potent Inhibition of Cryptococcus neoformans (Tue, 25 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00481
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Synthesis and Evaluation of Diphenyl Conjugated Imidazole Derivatives as Potential Glutaminyl Cyclase Inhibitors for Treatment of Alzheimer’s Disease (Tue, 25 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00648
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A Molecular Combination of Zinc(II) Phthalocyanine and Tamoxifen Derivative for Dual Targeting Photodynamic Therapy and Hormone Therapy (Mon, 24 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00682
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Recent Advances in Structure-Based Drug Design Targeting Class A G Protein-Coupled Receptors Utilizing Crystal Structures and Computational Simulations (Fri, 21 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01453
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Identification of Peptidic Antagonists of Vascular Endothelial Growth Factor Receptor 1 by Scanning the Binding Epitopes of Its Ligands (Fri, 21 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00283
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A Kinome-Wide Selective Radiolabeled TrkB/C Inhibitor for in Vitro and in Vivo Neuroimaging: Synthesis, Preclinical Evaluation, and First-in-Human (Fri, 21 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00396
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Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety (Thu, 20 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00833
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Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors (Thu, 20 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00662
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Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure (Wed, 19 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00285
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An Ursolic Acid Derived Small Molecule Triggers Cancer Cell Death through Hyperstimulation of Macropinocytosis (Wed, 19 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00592
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Potential Strategies to Target Protein–Protein Interactions in the DNA Damage Response and Repair Pathways (Wed, 12 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00358
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Identification of Three Novel Radiotracers for Imaging Aggregated Tau in Alzheimer’s Disease with Positron Emission Tomography (Wed, 12 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00632
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NMR Methods for Identification of False Positives in Biochemical Screens (Wed, 12 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01520
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Polyphenolic Phytochemicals in Cancer Prevention and Therapy: Bioavailability versus Bioefficacy (Tue, 11 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01026
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Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1 (Mon, 10 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00635
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Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents (Wed, 05 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01906
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Perspectives of Cannabinoid Type 2 Receptor (CB2R) Ligands in Neurodegenerative Disorders: Structure–Affinity Relationship (SAfiR) and Structure–Activity Relationship (SAR) Studies (Fri, 30 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00155
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In Silico Absorption, Distribution, Metabolism, Excretion, and Pharmacokinetics (ADME-PK): Utility and Best Practices. An Industry Perspective from the International Consortium for Innovation through Quality in Pharmaceutical Development (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00487
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Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8) (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00510
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Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00168
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Halogen Bonding in Nucleic Acid Complexes (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00329
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Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01912
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Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms (Tue, 20 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00215
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Compounds Interfering with Embryonic Lethal Abnormal Vision (ELAV) Protein–RNA Complexes: An Avenue for Discovering New Drugs (Mon, 19 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01871
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Correction to Past, Current, and Future Developments of Therapeutic Agents for Treatment of Chronic Hepatitis B Virus Infection (Wed, 14 Jun 2017)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00781
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Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances (Tue, 13 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01720
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Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins (Wed, 24 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01817
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Unusual Undergraduate Training in Medicinal Chemistry in Collaboration between Academia and Industry (Tue, 23 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00198
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Nitric Oxide Donor-Based Cancer Therapy: Advances and Prospects (Tue, 23 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01672
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Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases (Mon, 22 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00143
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Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective (Fri, 19 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00058
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Return of D4 Dopamine Receptor Antagonists in Drug Discovery (Wed, 17 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00151
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Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins (Wed, 10 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00413
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The Roles of Water in the Protein Matrix: A Largely Untapped Resource for Drug Discovery (Fri, 05 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00057
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Informing the Selection of Screening Hit Series with in Silico Absorption, Distribution, Metabolism, Excretion, and Toxicity Profiles (Fri, 05 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01577
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Synthetic Approaches to the New Drugs Approved During 2015 (Wed, 03 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00010
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Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ERα and ERβ Activity (Mon, 01 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01917
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Past, Current, and Future Developments of Therapeutic Agents for Treatment of Chronic Hepatitis B Virus Infection (Fri, 21 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01442
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A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos (Thu, 20 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01921
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Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals) (Mon, 17 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01872
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A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation (Mon, 17 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01781
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Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure–Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1 (Thu, 13 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01911
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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression (Fri, 24 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01816
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Regulating the Master Regulator: Controlling Ubiquitination by Thinking Outside the Active Site (Tue, 28 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01346
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