Journal of Medicinal Chemistry

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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Synthesis and in Vitro Evaluation of BBB Permeability, Tumor Cell Uptake, and Cytotoxicity of a Series of Carboranylporphyrin Conjugates (Thu, 31 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500786c
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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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Pyrrolo[3,2-b]quinoxaline Derivatives as Types I1/2 and II Eph Tyrosine Kinase Inhibitors: Structure-Based Design, Synthesis, and in Vivo Validation (Wed, 30 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5009242
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A Novel Class of Bis- and Tris-Chelate Diam(m)inebis(dicarboxylato)platinum(IV) Complexes as Potential Anticancer Prodrugs (Wed, 30 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500791c
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Synthesis of Tripeptides Containing d-Trp Substituted at the Indole Ring, Assessment of Opioid Receptor Binding and in Vivo Central Antinociception (Wed, 30 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5002925
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Structural Basis for Rational Design of Inhibitors Targeting Trypanosoma cruzi Sterol 14α-Demethylase: Two Regions of the Enzyme Molecule Potentiate Its Inhibition (Tue, 29 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500739f
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New Pyrrole Derivatives with Potent Tubulin Polymerization Inhibiting Activity As Anticancer Agents Including Hedgehog-Dependent Cancer (Tue, 29 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500561a
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Structure-Based Design and Synthesis of Antiparasitic Pyrrolopyrimidines Targeting Pteridine Reductase 1 (Tue, 29 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500483b
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Synthesis, Antimitotic and Antivascular Activity of 1-(3′,4′,5′-Trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles (Mon, 28 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5008193
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Discovery of 1-Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor (Mon, 28 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500496m
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Therapeutic Potential of Targeting the Oncogenic SHP2 Phosphatase (Mon, 28 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5006176
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Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8 (Fri, 25 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500871s
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First Photoswitchable Neurotransmitter Transporter Inhibitor: Light-Induced Control of γ-Aminobutyric Acid Transporter 1 (GAT1) Activity in Mouse Brain (Fri, 25 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5008566
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Anti-HIV Activities of Precisely Defined, Semirigid, Carboxylated Alternating Copolymers (Fri, 25 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401913w
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Discovery of Potent Cytotoxic Ortho-Aryl Chalcones as New Scaffold Targeting Tubulin and Mitosis with Affinity-Based Fluorescence (Fri, 25 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500024v
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Constrained Bithiazoles: Small Molecule Correctors of Defective ΔF508–CFTR Protein Trafficking (Fri, 25 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5007885
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Discovery of 1H-Indole-2-carboxamides as Novel Inhibitors of the Androgen Receptor Binding Function 3 (BF3) (Fri, 25 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500684r
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Studies Examining the Relationship between the Chemical Structure of Protoxin II and Its Activity on Voltage Gated Sodium Channels (Thu, 24 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500687u
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Discovery and Optimization of 1,3,5-Trisubstituted Pyrazolines as Potent and Highly Selective Allosteric Inhibitors of Protein Kinase C-ζ (Thu, 24 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500521n
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Discovery of a Novel, First-in-Class, Orally Bioavailable Azaindole Inhibitor (VX-787) of Influenza PB2 (Thu, 24 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5007275
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Correction to 4-Amino-1-hydroxy-2-oxo-1,8-naphthyridine-Containing Compounds Having High Potency against Raltegravir-Resistant Integrase Mutants of HIV-1 (Wed, 23 Jul 2014)
Journal of Medicinal Chemistry DOI: 10.1021/jm501059k
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Discovery of Glycine Sulfonamides as Dual Inhibitors of sn-1-Diacylglycerol Lipase α and α/β-Hydrolase Domain 6 (Wed, 23 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500681z
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[111In-DOTA]LTT-SS28, a First Pansomatostatin Radioligand for in Vivo Targeting of Somatostatin Receptor-Positive Tumors (Wed, 23 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500581d
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N-Tetradecylcarbamyl Lipopeptides as Novel Agonists for Toll-like Receptor 2 (Wed, 23 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500722p
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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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N-Aryl-2-aminobenzimidazoles: Novel, Efficacious, Antimalarial Lead Compounds (Mon, 21 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500715u
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Modification and Biological Evaluation of Thiazole Derivatives as Novel Inhibitors of Metastatic Cancer Cell Migration and Invasion (Fri, 18 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500724x
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Discovery of Selective Hexapeptide Agonists to Human Neuromedin U Receptors Types 1 and 2 (Fri, 18 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500599s
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Putative Kappa Opioid Heteromers As Targets for Developing Analgesics Free of Adverse Effects (Fri, 18 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500159d
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Pyridyl Benzamides as a Novel Class of Potent Inhibitors for the Kinetoplastid Trypanosoma brucei (Thu, 17 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500191u
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Method for the Evaluation of Structure–Activity Relationship Information Associated with Coordinated Activity Cliffs (Thu, 17 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500577n
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Indazole- and Indole-5-carboxamides: Selective and Reversible Monoamine Oxidase B Inhibitors with Subnanomolar Potency (Wed, 16 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500729a
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Development and Biological Evaluation of Potent and Selective c-KITD816V Inhibitors (Wed, 16 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500413g
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Diarylthiazole: An Antimycobacterial Scaffold Potentially Targeting PrrB-PrrA Two-Component System (Wed, 16 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500833f
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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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Toward Fluorescent Probes for G-Protein-Coupled Receptors (GPCRs) (Thu, 10 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401823z
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Ado-trastuzumab Emtansine (T-DM1): An Antibody–Drug Conjugate (ADC) for HER2-Positive Breast Cancer (Thu, 10 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500766w
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Discovery of a Small Molecule MDM2 Inhibitor (AMG 232) for Treating Cancer (Wed, 09 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500627s
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Targeting the Androgen Receptor with Steroid Conjugates (Tue, 08 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500101h
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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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Recent Developments in Novel Antidepressants Targeting α4β2-Nicotinic Acetylcholine Receptors (Wed, 02 Jul 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401937a
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Polypharmacology: Challenges and Opportunities in Drug Discovery (Wed, 25 Jun 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5006463
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Calcitonin Gene-Related Peptide Receptor Antagonists: New Therapeutic Agents for Migraine (Tue, 24 Jun 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500364u
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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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Development of Synthetic Lethality Anticancer Therapeutics (Fri, 13 Jun 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500415t
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Elements and Modulation of Functional Dynamics (Tue, 10 Jun 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500325k
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Physicochemical Descriptors of Aromatic Character and Their Use in Drug Discovery (Tue, 03 Jun 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500515d
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Serotonin 5-HT6 Receptor Antagonists for the Treatment of Cognitive Deficiency in Alzheimer’s Disease (Tue, 03 Jun 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5003952
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From Chemical Tools to Clinical Medicines: Nonimmunosuppressive Cyclophilin Inhibitors Derived from the Cyclosporin and Sanglifehrin Scaffolds (Tue, 03 Jun 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500223x
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The Medicinal Chemistry of Liver X Receptor (LXR) Modulators (Wed, 28 May 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500442z
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Small Molecule Inhibitors Targeting Activator Protein 1 (AP-1) (Tue, 27 May 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5004733
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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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Biased Ligand Modulation of Seven Transmembrane Receptors (7TMRs): Functional Implications for Drug Discovery (Tue, 29 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401677g
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Successes and Challenges in Phenotype-Based Lead Discovery for Prion Diseases (Thu, 24 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5001425
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Nucleotide-Binding Oligomerization Domain (NOD) Inhibitors: A Rational Approach toward Inhibition of NOD Signaling Pathway (Tue, 22 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401841p
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Motor Neuron Disease: A Chemical Perspective (Thu, 17 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5001584
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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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Functional Probes of Drug–Receptor Interactions Implicated by Structural Studies: Cys-Loop Receptors Provide a Fertile Testing Ground (Mon, 10 Mar 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500023m
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Strategies To Inhibit Tumor Associated Integrin Receptors: Rationale for Dual and Multi-Antagonists (Fri, 07 Mar 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5000547
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Hydrocarbon-Stapled Peptides: Principles, Practice, and Progress (Thu, 06 Mar 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4011675
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