Journal of Medicinal Chemistry

Synthesis and Biological Evaluation of Novel Peptide BF2 as an Antibacterial Agent against Clinical Isolates of Vancomycin-Resistant Enterococci (Wed, 29 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500960s
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Evidence for Targeting Thioredoxin Reductases with Ferrocenyl Quinone Methides. A Possible Molecular Basis for the Antiproliferative Effect of Hydroxyferrocifens on Cancer Cells (Tue, 28 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5013165
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Second-Generation Antibacterial Benzimidazole Ureas: Discovery of a Preclinical Candidate with Reduced Metabolic Liability (Tue, 28 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500563g
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Structure–Activity Relationship of Highly Potent Galactonoamidine Inhibitors toward β-Galactosidase (Aspergillus oryzae) (Mon, 27 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501111y
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Radiosynthesis and Evaluation of an 18F-Labeled Positron Emission Tomography (PET) Radioligand for Metabotropic Glutamate Receptor Subtype 4 (mGlu4) (Mon, 27 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501245b
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Potent Cholesteryl Ester Transfer Protein Inhibitors of Reduced Lipophilicity: 1,1′-Spiro-Substituted Hexahydrofuroquinoline Derivatives (Mon, 27 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500431d
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Two-Pronged Attack: Dual Inhibition of Plasmodium falciparum M1 and M17 Metalloaminopeptidases by a Novel Series of Hydroxamic Acid-Based Inhibitors (Fri, 24 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501323a
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Discovery of Dual Leucine Zipper Kinase (DLK, MAP3K12) Inhibitors with Activity in Neurodegeneration Models (Thu, 23 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5013984
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Targeting Nucleus DNA with a Cyclometalated Dipyridophenazineruthenium(II) Complex (Thu, 23 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501095r
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Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 2 (Thu, 23 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500887k
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Discovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase (Wed, 22 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500847m
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Orally Bioavailable 6-Chloro-7-methoxy-4(1H)-quinolones Efficacious against Multiple Stages of Plasmodium (Wed, 22 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500942v
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Oligonucleotide Analogues as Modulators of the Expression and Function of Noncoding RNAs (ncRNAs): Emerging Therapeutics Applications (Tue, 21 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5006594
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Trehalose- and Glucose-Derived Glycoamphiphiles: Small-Molecule and Nanoparticle Toll-Like Receptor 4 (TLR4) Modulators (Tue, 21 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501182w
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Nonpeptide Small Molecule Agonist and Antagonist Original Leads for Neuropeptide FF1 and FF2 Receptors (Tue, 21 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500989n
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Binding Modes of Reverse Fosmidomycin Analogs toward the Antimalarial Target IspC (Mon, 20 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500850y
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Inhibitory Activities of Propolis and Its Promising Component, Caffeic Acid Phenethyl Ester, against Amyloidogenesis of Human Transthyretin (Mon, 20 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500997m
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Identification and Development of Biphenyl Substituted Iminosugars as Improved Dual Glucosylceramide Synthase/Neutral Glucosylceramidase Inhibitors (Fri, 17 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501181z
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Structural Insights on Carbonic Anhydrase Inhibitory Action, Isoform Selectivity, and Potency of Sulfonamides and Coumarins Incorporating Arylsulfonylureido Groups (Fri, 17 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501314c
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Novel DNA Gyrase Inhibiting Spiropyrimidinetriones with a Benzisoxazole Scaffold: SAR and in Vivo Characterization (Fri, 17 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501174m
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Synthesis and Biological Evaluation of a Novel Series of Heterobivalent Muscarinic Ligands Based on Xanomeline and 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) (Thu, 16 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501173q
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Converting Potent Indeno[1,2-b]indole Inhibitors of Protein Kinase CK2 into Selective Inhibitors of the Breast Cancer Resistance Protein ABCG2 (Thu, 16 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500943z
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Substitution of the Lys Linker with the β-Ala Linker Dramatically Decreased the Renal Uptake of 99mTc-Labeled Arg-X-Asp-Conjugated and X-Ala-Asp-Conjugated α-Melanocyte Stimulating Hormone Peptides (Thu, 16 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501114v
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CB2-Selective Cannabinoid Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Modeling Investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides (Wed, 15 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500807e
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DNA Repair and Redox Activities and Inhibitors of Apurinic/Apyrimidinic Endonuclease 1/Redox Effector Factor 1 (APE1/Ref-1): A Comparative Analysis and Their Scope and Limitations toward Anticancer Drug Development (Wed, 15 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500865u
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Discovery of Novel, Highly Potent, and Selective Quinazoline-2-carboxamide-Based Matrix Metalloproteinase (MMP)-13 Inhibitors without a Zinc Binding Group Using a Structure-Based Design Approach (Wed, 15 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500981k
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Synthesis and Preclinical Evaluation of 2-(2-Furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine ([11C]Preladenant) as a PET Tracer for the Imaging of Cerebral Adenosine A2A Receptors (Wed, 15 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501065t
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Design, Synthesis, and Antibacterial Properties of Dual-Ligand Inhibitors of Acetyl-CoA Carboxylase (Wed, 15 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501082n
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Targeting Matrix Metalloproteinases: Exploring the Dynamics of the S1′ Pocket in the Design of Selective, Small Molecule Inhibitors (Fri, 10 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500505f
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Optimized Protein Kinase Cθ (PKCθ) Inhibitors Reveal Only Modest Anti-inflammatory Efficacy in a Rodent Model of Arthritis (Thu, 09 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5013006
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Discovery and Characterization of MAPK-activated Protein Kinase-2 Prevention of Activation Inhibitors (Thu, 09 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501038s
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Importance of Purity Evaluation and the Potential of Quantitative 1H NMR as a Purity Assay (Wed, 08 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500734a
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Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals (Tue, 07 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501100b
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Beyond C, H, O, and N! Analysis of the Elemental Composition of U.S. FDA Approved Drug Architectures (Mon, 06 Oct 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501105n
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Development of Inhibitors of the 2C-Methyl-d-erythritol 4-Phosphate (MEP) Pathway Enzymes as Potential Anti-Infective Agents (Thu, 25 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5010978
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Peptides Containing β-Amino Acid Patterns: Challenges and Successes in Medicinal Chemistry (Wed, 24 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5010896
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Acidic and Basic Drugs in Medicinal Chemistry: A Perspective (Thu, 18 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501000a
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Exploring the Scaffold Universe of Kinase Inhibitors (Tue, 16 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501237k
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Design, Synthesis, and Evaluation of Novel Imidazo[1,2-a][1,3,5]triazines and Their Derivatives as Focal Adhesion Kinase Inhibitors with Antitumor Activity (Thu, 11 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500784e
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Positron Emission Tomography in CNS Drug Discovery and Drug Monitoring (Wed, 10 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5001858
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Natural Products in Medicine: Transformational Outcome of Synthetic Chemistry (Wed, 10 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500941m
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Desferrithiocin: A Search for Clinically Effective Iron Chelators (Wed, 10 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500828f
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“New Drug” Designations for New Therapeutic Entities: New Active Substance, New Chemical Entity, New Biological Entity, New Molecular Entity (Thu, 04 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm402001w
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Medicinal Chemistry of Catechol O-Methyltransferase (COMT) Inhibitors and Their Therapeutic Utility (Tue, 02 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500572b
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Progress in the Discovery and Development of Heat Shock Protein 90 (Hsp90) Inhibitors (Fri, 29 Aug 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500823a
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Small Molecule Adenosine 5′-Monophosphate Activated Protein Kinase (AMPK) Modulators and Human Diseases (Thu, 28 Aug 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401994c
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Small Molecule Ghrelin Receptor Inverse Agonists and Antagonists (Wed, 06 Aug 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5003183
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Comprehensive Analysis of Three-Dimensional Activity Cliffs Formed by Kinase Inhibitors with Different Binding Modes and Cliff Mapping of Structural Analogues (Thu, 31 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5009264
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Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2) (Wed, 30 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500480k
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Current Compound Coverage of the Kinome (Wed, 30 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5008159
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Optimization of Potent DFG-in Inhibitors of Platelet Derived Growth Factor Receptorβ (PDGF-Rβ) Guided by Water Thermodynamics (Mon, 21 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500373x
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Development of First Lead Structures for Phosphoinositide 3-Kinase-C2γ Inhibitors (Mon, 14 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5006034
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Discovery of Selective and Orally Bioavailable Protein Kinase Cθ (PKCθ) Inhibitors from a Fragment Hit (Mon, 07 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500669m
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The Discovery of Polo-Like Kinase 4 Inhibitors: Identification of (1R,2S)-2-(3-((E)-4-(((cis)-2,6-Dimethylmorpholino)methyl)styryl)-1H-indazol-6-yl)-5′-methoxyspiro[cyclopropane-1,3′-indolin]-2′-one (CFI-400945) as a Potent, Orally Active Antitumor Agent (Tue, 24 Jun 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5005336
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Discovery of Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent Inhibitory Activities against Both Wild-type and Mutant ALK Kinases (Thu, 08 May 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5005144
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Structural Basis for Isoform Selectivity in a Class of Benzothiazole Inhibitors of Phosphoinositide 3-Kinase γ (Fri, 02 May 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500362j
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Structure-Based Drug Design of RN486, a Potent and Selective Bruton’s Tyrosine Kinase (BTK) Inhibitor, for the Treatment of Rheumatoid Arthritis (Wed, 16 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500305p
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