Journal of Medicinal Chemistry

Optimizing Protonation States for Selective Double-Strand DNA Photocleavage in Hypoxic Tumors: pH-Gated Transitions of Lysine Dipeptides (Wed, 31 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01164
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Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors (Tue, 30 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00697
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Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I “Gatekeeper” Mutant of cKIT Kinase (Tue, 30 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00902
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Synthesis and Biological Evaluation of N-[2-(4-Hydroxyphenylamino)-pyridin-3-yl]-4-methoxy-benzenesulfonamide (ABT-751) Tricyclic Analogues as Antimitotic and Antivascular Agents with Potent in Vivo Antitumor Activity (Tue, 30 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00847
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Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux (Tue, 30 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00867
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Purine-Type Compounds Induce Microtubule Fragmentation and Lung Cancer Cell Death through Interaction with Katanin (Tue, 30 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00797
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Structure–Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance (Tue, 30 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01050
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Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD) (Mon, 29 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00753
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Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors (Mon, 29 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00425
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Identification of Inhibitors for the DEDDh Family of Exonucleases and a Unique Inhibition Mechanism by Crystal Structure Analysis of CRN-4 Bound with 2-Morpholin-4-ylethanesulfonate (MES) (Mon, 29 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00794
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Design, Synthesis, and Bioactivation of O-Glycosylated Prodrugs of the Natural Nitric Oxide Precursor Nω-Hydroxy-l-arginine (Mon, 29 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00810
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Apo- and Antagonist-Binding Structures of Vitamin D Receptor Ligand-Binding Domain Revealed by Hybrid Approach Combining Small-Angle X-ray Scattering and Molecular Dynamics (Fri, 26 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00682
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Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles (Fri, 26 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00738
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Small Molecule Reversible Inhibitors of Bruton’s Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177) (Fri, 26 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00722
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Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis (Fri, 26 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00594
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Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing (Fri, 26 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00821
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Small Antimicrobial Agents Based on Acylated Reduced Amide Scaffold (Thu, 25 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00640
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Hit-to-Lead Studies for the Antimalarial Tetrahydroisoquinolone Carboxanilides (Thu, 25 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00752
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Pyridyl-alanine as a Hydrophilic, Aromatic Element in Peptide Structural Optimization (Thu, 25 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00840
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Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153) (Wed, 24 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00070
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Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells (Wed, 24 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00772
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Discovery, Synthesis, and Evaluation of 2,4-Diaminoquinazolines as a Novel Class of Pancreatic β-Cell-Protective Agents against Endoplasmic Reticulum (ER) Stress (Tue, 23 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00041
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Development of a High-Affinity PET Radioligand for Imaging Cannabinoid Subtype 2 Receptor (Tue, 23 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00554
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Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus (Tue, 23 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00747
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A Selective Galactose–Coumarin-Derived Galectin-3 Inhibitor Demonstrates Involvement of Galectin-3-glycan Interactions in a Pulmonary Fibrosis Model (Tue, 23 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00957
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1,2-Benzisoselenazol-3(2H)-one Derivatives As a New Class of Bacterial Urease Inhibitors (Mon, 22 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00986
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Correction to Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease (Mon, 22 Aug 2016)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01157
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Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family (Mon, 22 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00883
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Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy (Sat, 20 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00866
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Human Toll-like Receptor (TLR) 8-Specific Agonistic Activity in Substituted Pyrimidine-2,4-diamines (Fri, 19 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00872
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Effects of 5-O-Ribosylation of Aminoglycosides on Antimicrobial Activity and Selective Perturbation of Bacterial Translation (Fri, 19 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00793
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Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension (Fri, 19 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00703
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Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm (Fri, 19 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00764
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Allosteric Modulation of Phosphatase Activity May Redefine Therapeutic Value (Fri, 19 Aug 2016)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01210
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Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6) (Thu, 18 Aug 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00869
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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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Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor (Tue, 12 Jul 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00680
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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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Endothelin-Receptor Antagonists beyond Pulmonary Arterial Hypertension: Cancer and Fibrosis (Wed, 15 Jun 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01781
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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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β-Lactamases: Why and How (Fri, 27 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00448
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Carbon Nanotubes in Biomedical Applications: Factors, Mechanisms, and Remedies of Toxicity (Fri, 27 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01770
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Design Principles for Fragment Libraries: Maximizing the Value of Learnings from Pharma Fragment-Based Drug Discovery (FBDD) Programs for Use in Academia (Mon, 16 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00197
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Challenges and Opportunities for the Application of Boron Clusters in Drug Design (Tue, 10 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01932
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From Companion Diagnostics to Theranostics: A New Avenue for Alzheimer’s Disease? (Fri, 06 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00151
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Polymerase Acidic Protein–Basic Protein 1 (PA–PB1) Protein–Protein Interaction as a Target for Next-Generation Anti-influenza Therapeutics (Tue, 19 Apr 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01474
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Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases (Mon, 18 Apr 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01516
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