Journal of Medicinal Chemistry

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300 (Wed, 28 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01022
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Correction to Design and Synthesis of Highly Potent and Isoform Selective JNK3 Inhibitors: SAR Studies on Aminopyrazole Derivatives (Tue, 27 Sep 2016)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01369
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Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors (Tue, 27 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00774
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A Novel Parkinson’s Disease Drug Candidate with Potent Anti-neuroinflammatory Effects through the Src Signaling Pathway (Tue, 27 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00976
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Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis (Tue, 27 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00355
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Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist (Tue, 27 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01071
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Identification of Ligand Binding Hot Spots of the Histamine H1 Receptor following Structure-Based Fragment Optimization (Tue, 27 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00981
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Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer’s Disease (Tue, 27 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00908
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Development of Therapeutics That Induce Mitochondrial Biogenesis for the Treatment of Acute and Chronic Degenerative Diseases (Tue, 27 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00669
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Nucleoside Derived Antibiotics to Fight Microbial Drug Resistance: New Utilities for an Established Class of Drugs? (Tue, 27 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00325
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The Rational Design, Synthesis, and Antimicrobial Properties of Thiophene Derivatives That Inhibit Bacterial Histidine Kinases (Mon, 26 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00580
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Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208) (Thu, 22 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00420
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Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity (Thu, 22 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00685
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Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1 (Thu, 22 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00461
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Discovery and Optimization of 1-Phenoxy-2-aminoindanes as Potent, Selective, and Orally Bioavailable Inhibitors of the Na+/H+ Exchanger Type 3 (NHE3) (Thu, 22 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00624
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Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility (Wed, 21 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00379
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Optimization and Structure–Activity Relationships of Phosphinic Pseudotripeptide Inhibitors of Aminopeptidases That Generate Antigenic Peptides (Tue, 20 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01031
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A Lipophilic Pt(IV) Oxaliplatin Derivative Enhances Antitumor Activity (Tue, 20 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00955
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Enabling Efficient Positron Emission Tomography (PET) Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) with a Robust and One-Step Radiosynthesis of a Highly Potent 18F-Labeled Ligand ([18F]UCB-H) (Tue, 20 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00905
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Amending HIV Drugs: A Novel Small-Molecule Approach To Target Lupus Anti-DNA Antibodies (Tue, 20 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00694
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Discovery of Benzothiazole Scaffold-Based DNA Gyrase B Inhibitors (Tue, 20 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00864
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Structure–Activity Relationships and Kinetic Studies of Peptidic Antagonists of CBX Chromodomains (Mon, 19 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00801
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Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides (Mon, 19 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00442
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Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers (Mon, 19 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01088
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Synthesis and Enantiomeric Separation of a Novel Spiroketal Derivative: A Potent Human Telomerase Inhibitor with High in Vitro Anticancer Activity (Mon, 19 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01046
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Modeling, Synthesis, and Biological Evaluation of Potential Retinoid X Receptor (RXR)-Selective Agonists: Analogues of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and 6-(Ethyl(5,5,8,8-tetrahydronaphthalen-2-yl)amino)nicotinic Acid (NEt-TMN) (Mon, 19 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00812
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β-Sulfonamido Functionalized Aspartate Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype Selectivity Profiles Arising from Subtle Structural Differences (Fri, 16 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01066
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Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor (Thu, 15 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00676
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Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6 (Thu, 15 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01033
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Truncated Autoinducing Peptides as Antagonists of Staphylococcus lugdunensis Quorum Sensing (Thu, 15 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00727
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Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure–Activity Relationship Study (Wed, 14 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01058
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Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor (Mon, 12 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00995
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Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy (Sat, 10 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00723
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Nucleoside Phosphate and Phosphonate Prodrug Clinical Candidates (Thu, 08 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00523
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Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective (Wed, 07 Sep 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00438
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Driving Structure-Based Drug Discovery through Cosolvent Molecular Dynamics (Wed, 17 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00399
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Small Molecules in Development for the Treatment of Spinal Muscular Atrophy (Tue, 16 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00670
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Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer (Wed, 03 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00618
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Drug-like Antagonists of P2Y ReceptorsFrom Lead Identification to Drug Development (Mon, 01 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01972
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Transient Receptor Potential Melastatin 8 Channel (TRPM8) Modulation: Cool Entryway for Treating Pain and Cancer (Mon, 01 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00305
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Therapeutic Potential of Foldamers: From Chemical Biology Tools To Drug Candidates? (Fri, 29 Jul 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00376
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The Medicinal Chemistry of Therapeutic Oligonucleotides (Fri, 29 Jul 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00551
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An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy (Wed, 27 Jul 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00055
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Peptidyl-Proline Isomerases (PPIases): Targets for Natural Products and Natural Product-Inspired Compounds (Mon, 25 Jul 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00411
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Targeting the Translesion Synthesis Pathway for the Development of Anti-Cancer Chemotherapeutics (Tue, 19 Jul 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00596
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Underexplored Opportunities for Natural Products in Drug Discovery (Mon, 11 Jul 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00473
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G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives (Fri, 08 Jul 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01939
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The “Cyclopropyl Fragment” is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules (Thu, 30 Jun 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00472
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Blocking Blood Flow to Solid Tumors by Destabilizing Tubulin: An Approach to Targeting Tumor Growth (Mon, 27 Jun 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00463
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Metabolomics as a Challenging Approach for Medicinal Chemistry and Personalized Medicine (Mon, 27 Jun 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01335
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Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy (Fri, 03 Jun 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00150
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