Journal of Medicinal Chemistry

Peptide Inhibitors of the Escherichia coli DsbA Oxidative Machinery Essential for Bacterial Virulence (Thu, 18 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500955s
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RXR Partial Agonist Produced by Side Chain Repositioning of Alkoxy RXR Full Agonist Retains Antitype 2 Diabetes Activity without the Adverse Effects (Wed, 17 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501863r
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Iterative Conversion of Cyclin Binding Groove Peptides into Druglike CDK Inhibitors with Antitumor Activity (Wed, 17 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5015023
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Evaluation of Three Different Families of Bombesin Receptor Radioantagonists for Targeted Imaging and Therapy of Gastrin Releasing Peptide Receptor (GRP-R) Positive Tumors (Wed, 17 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5012066
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Amino Acid Modified Xanthone Derivatives: Novel, Highly Promising Membrane-Active Antimicrobials for Multidrug-Resistant Gram-Positive Bacterial Infections (Wed, 17 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501285x
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A Conjugate Vaccine Using Enantiopure Hapten Imparts Superior Nicotine-Binding Capacity (Wed, 17 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501625j
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Probing the Carboxyester Side Chain in Controlled Deactivation (−)-Δ8-Tetrahydrocannabinols (Tue, 16 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501165d
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Optimization of Sphingosine-1-phosphate-1 Receptor Agonists: Effects of Acidic, Basic, and Zwitterionic Chemotypes on Pharmacokinetic and Pharmacodynamic Profiles (Mon, 15 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5010336
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Correction to Substrate-Based Fragment Identification for the Development of Selective, Nonpeptidic Inhibitors of Striatal-Enriched Protein Tyrosine Phosphatase (Fri, 12 Dec 2014)
Journal of Medicinal Chemistry DOI: 10.1021/jm5018847
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Design of Chemically Stable, Potent, and Efficacious MDM2 Inhibitors That Exploit the Retro-Mannich Ring-Opening-Cyclization Reaction Mechanism in Spiro-oxindoles (Fri, 12 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501541j
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Conformational Analysis of the DFG-Out Kinase Motif and Biochemical Profiling of Structurally Validated Type II Inhibitors (Fri, 12 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501603h
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Synthesis and Structure–Activity Relationship Studies of Small Molecule Disruptors of EWS-FLI1 Interactions in Ewing’s Sarcoma (Fri, 12 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501372p
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Design and Synthesis of Pironetin Analogue/Colchicine Hybrids and Study of Their Cytotoxic Activity and Mechanisms of Interaction with Tubulin (Fri, 12 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501112q
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Selection of Fragments for Kinase Inhibitor Design: Decoration Is Key (Fri, 12 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501597j
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Discovery of 2-(Cyclohexylmethylamino)pyrimidines as a New Class of Reversible Valosine Containing Protein Inhibitors (Fri, 12 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501313x
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Decreasing the Rate of Metabolic Ketone Reduction in the Discovery of a Clinical Acetyl-CoA Carboxylase Inhibitor for the Treatment of Diabetes (Thu, 11 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5016022
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Synthesis and κ-Opioid Receptor Activity of Furan-Substituted Salvinorin A Analogues (Tue, 09 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501521d
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Discovery of Cytotoxic Dolastatin 10 Analogues with N-Terminal Modifications (Tue, 09 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501649k
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Advancing the Kinase Field: New Targets and Second Generation Inhibitors (Tue, 09 Dec 2014)
Journal of Medicinal Chemistry DOI: 10.1021/jm5018708
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Synthesis, Antitumor Activity, and Mechanism of Action of Benzo[b]chromeno[6,5-g][1,8]naphthyridin-7-one Analogs of Acronycine (Tue, 09 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500927d
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G-Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5) Agonists Reduce the Production of Proinflammatory Cytokines and Stabilize the Alternative Macrophage Phenotype (Tue, 09 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501052c
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Synthesis of Gallinamide A Analogues as Potent Falcipain Inhibitors and Antimalarials (Mon, 08 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501439w
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Inhibitors of c-Jun N-Terminal Kinases: An Update (Mon, 08 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501212r
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Synthesis and Biological Evaluation of Pentacyclic Strychnos Alkaloids as Selective Modulators of the ABCC10 (MRP7) Efflux Pump (Mon, 08 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501189p
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Discovery of a Phosphodiesterase 9A Inhibitor as a Potential Hypoglycemic Agent (Mon, 08 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500836h
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N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a New Cholinesterase and Monoamine Oxidase Dual Inhibitor (Mon, 08 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501501a
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Antiadhesive Properties of Glycoclusters against Pseudomonas aeruginosa Lung Infection (Mon, 08 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500038p
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Identification of Potent and Selective Hydantoin Inhibitors of Aggrecanase-1 and Aggrecanase-2 That Are Efficacious in Both Chemical and Surgical Models of Osteoarthritis (Fri, 05 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501522n
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Phosphatidylinositol 3-Kinase (PI3K) and Phosphatidylinositol 3-Kinase-Related Kinase (PIKK) Inhibitors: Importance of the Morpholine Ring (Fri, 05 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501026z
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Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders (Fri, 05 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5016044
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Novel Insights into Structure and Function of Factor XIIIa-Inhibitor Tridegin (Fri, 05 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501058g
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Tetra-Substituted Pyridinylimidazoles As Dual Inhibitors of p38α Mitogen-Activated Protein Kinase and c-Jun N-Terminal Kinase 3 for Potential Treatment of Neurodegenerative Diseases (Fri, 05 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501557a
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Optimization of Potent and Selective Quinazolinediones: Inhibitors of Respiratory Syncytial Virus That Block RNA-Dependent RNA-Polymerase Complex Activity (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500902x
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Targeting DNA Methylation with Small Molecules: What’s Next? (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500843d
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Synthesis and Biological Evaluation of Novel Sigma-1 Receptor Antagonists Based on Pyrimidine Scaffold As Agents for Treating Neuropathic Pain (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501207r
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Electrophilic Warhead-Based Design of Compounds Preventing NLRP3 Inflammasome-Dependent Pyroptosis (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501072b
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Synthesis, in Vitro Evaluation and Cocrystal Structure of 4-Oxo-[1]benzopyrano[4,3-c]pyrazole Cryptosporidium parvum Inosine 5′-Monophosphate Dehydrogenase (CpIMPDH) Inhibitors (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501527z
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Parallel Worlds of Public and Commercial Bioactive Chemistry Data (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5011308
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Discovery of AM-7209, a Potent and Selective 4-Amidobenzoic Acid Inhibitor of the MDM2–p53 Interaction (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501550p
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Inhibitors of p21-Activated Kinases (PAKs) (Wed, 03 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501613q
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Discovery and in Vivo Evaluation of (S)-N-(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and Related PI3Kδ Inhibitors for Inflammation and Autoimmune Disease (Wed, 03 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501624r
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Combining X-ray Crystallography and Molecular Modeling toward the Optimization of Pyrazolo[3,4-d]pyrimidines as Potent c-Src Inhibitors Active in Vivo against Neuroblastoma (Wed, 03 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5013159
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Internalization and Stability of a Thymidylate Synthase Peptide Inhibitor in Ovarian Cancer Cells (Wed, 03 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501397h
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Selective Inhibitors of Protein Methyltransferases (Tue, 02 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501234a
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Discovery of (2S)-8-[(3R)-3-Methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: A Novel Potent and Selective Inhibitor of Vps34 for the Treatment of Solid Tumors (Wed, 26 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5013352
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SAR156497, an Exquisitely Selective Inhibitor of Aurora Kinases (Mon, 24 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501326k
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Targeting Aldose Reductase for the Treatment of Diabetes Complications and Inflammatory Diseases: New Insights and Future Directions (Mon, 17 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500907a
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Discovery and Preclinical Profiling of 3-[4-(Morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor (Mon, 17 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5014055
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Inhibiting the Deubiquitinating Enzymes (DUBs) (Fri, 14 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501061a
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Small-Molecule Inhibitors of the MDM2–p53 Protein–Protein Interaction (MDM2 Inhibitors) in Clinical Trials for Cancer Treatment (Fri, 14 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501092z
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Development of Organometallic S6K1 Inhibitors (Thu, 13 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5011868
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Glucagon-like Peptide-1 (GLP-1) Analogs: Recent Advances, New Possibilities, and Therapeutic Implications (Thu, 13 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500810s
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A New Class of Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1 (Wed, 05 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501147g
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Recent Advances in the Development of Acetyl-CoA Carboxylase (ACC) Inhibitors for the Treatment of Metabolic Disease (Mon, 03 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500695e
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FPR2/ALXR Agonists and the Resolution of Inflammation (Mon, 03 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501051x
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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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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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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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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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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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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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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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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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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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