Journal of Medicinal Chemistry

Amphipathicity Determines Different Cytotoxic Mechanisms of Lysine- or Arginine-Rich Cationic Hydrophobic Peptides in Cancer Cells (Thu, 26 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b02016
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Synthesis, Radiolabeling, and Biological Evaluation of 5-Hydroxy-2-[18F]fluoroalkyl-tryptophan Analogues as Potential PET Radiotracers for Tumor Imaging (Thu, 26 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00057
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Quantitative Assessment of the Impact of Fluorine Substitution on P-Glycoprotein (P-gp) Mediated Efflux, Permeability, Lipophilicity, and Metabolic Stability (Thu, 26 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00027
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Targeted Nanoparticles for the Delivery of Novel Bioactive Molecules to Pancreatic Cancer Cells (Thu, 26 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01571
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Thiolactomycin-Based Inhibitors of Bacterial β-Ketoacyl-ACP Synthases with in Vivo Activity (Tue, 24 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00236
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Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities (Tue, 24 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00579
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Synthesis and Biological Evaluation of 4-Anilino-quinazolines and -quinolines as Inhibitors of Breast Cancer Resistance Protein (ABCG2) (Tue, 24 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00330
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Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window (Tue, 24 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00638
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Twenty Crystal Structures of Bromodomain and PHD Finger Containing Protein 1 (BRPF1)/Ligand Complexes Reveal Conserved Binding Motifs and Rare Interactions (Tue, 24 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00215
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Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors (Tue, 24 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00029
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Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo (Mon, 23 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00021
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Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737) (Mon, 23 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01938
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An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C (Mon, 23 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00443
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Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity? (Mon, 23 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00585
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Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity (Sat, 21 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00275
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Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site (Fri, 20 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00071
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Screening and Design of Inhibitor Scaffolds for the Antibiotic Resistance Oxacillinase-48 (OXA-48) through Surface Plasmon Resonance Screening (Fri, 20 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00660
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Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X-ray Fragment Screening (Fri, 20 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00212
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Inducing Protein Degradation as a Therapeutic Strategy (Fri, 20 May 2016)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00735
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Near-Infrared Illumination of Native Tissues for Image-Guided Surgery (Thu, 19 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00038
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Passive Membrane Permeability of Macrocycles Can Be Controlled by Exocyclic Amide Bonds (Thu, 19 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00222
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Rational Design of Calpain Inhibitors Based on Calpastatin Peptidomimetics (Wed, 18 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00267
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Targeting the Motion of Shikimate Kinase: Development of Competitive Inhibitors that Stabilize an Inactive Open Conformation of the Enzyme (Wed, 18 May 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00483
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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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Structural Basis for the Selective Binding of Inhibitors to 6-Hydroxymethyl-7,8-dihydropterin Pyrophosphokinase from Staphylococcus aureus and Escherichia coli (Tue, 26 Apr 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00002
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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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Artemisinin-Derived Dimers: Potent Antimalarial and Anticancer Agents (Wed, 06 Apr 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01380
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Gamma Secretase Modulators: New Alzheimer’s Drugs on the Horizon? (Tue, 05 Apr 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01960
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Ten Years of Medicinal Chemistry (2005–2014) in the Journal of Medicinal Chemistry: Country of Contributors, Topics, and Public–Private Partnerships (Tue, 05 Apr 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01349
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Integrating Everything: The Molecule Selection Toolkit, a System for Compound Prioritization in Drug Discovery (Tue, 22 Mar 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01338
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PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design (Fri, 18 Mar 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01813
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Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility (Mon, 14 Mar 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01499
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Targeting the Bacterial Division Protein FtsZ (Thu, 10 Mar 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01098
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An Overview of Severe Acute Respiratory Syndrome–Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy (Mon, 29 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01461
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Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases (Mon, 29 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00342
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Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer (Fri, 26 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00840
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Chemical Space of DNA-Encoded Libraries (Thu, 25 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01874
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Design and Development of Microsomal Prostaglandin E2 Synthase-1 Inhibitors: Challenges and Future Directions (Wed, 24 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01750
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Lanthanides: Applications in Cancer Diagnosis and Therapy (Fri, 19 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01975
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Novel Strategies for the Treatment of Pseudomonas aeruginosa Infections (Thu, 18 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01698
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Quadruplex Nucleic Acids as Novel Therapeutic Targets (Tue, 16 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01835
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Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90–Kinase Interactions (Tue, 16 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01106
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Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action (Tue, 09 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01485
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The Medicinal Chemistry of Dengue Virus (Fri, 05 Feb 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01653
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Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature (Thu, 28 Jan 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01599
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Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS (Fri, 22 Jan 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01697
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Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure–Function Perspective (Tue, 19 Jan 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01281
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Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K+ Channel 1). A Novel Therapeutic Target? (Mon, 14 Dec 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00671
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Protein-Observed Fluorine NMR: A Bioorthogonal Approach for Small Molecule Discovery (Mon, 14 Dec 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01447
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