Journal of Medicinal Chemistry

Synthesis and Biological Evaluation of Novel Allosteric Enhancers of the A1 Adenosine Receptor Based on 2-Amino-3-(4′-Chlorobenzoyl)-4-Substituted-5-Arylethynyl Thiophene (Fri, 12 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5008853
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Discovery of Dual Death-Associated Protein Related Apoptosis Inducing Protein Kinase 1 and 2 Inhibitors by a Scaffold Hopping Approach (Thu, 11 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5007929
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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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Novel Nitric Oxide-Releasing Derivatives of Brusatol as Anti-Inflammatory Agents: Design, Synthesis, Biological Evaluation, and Nitric Oxide Release Studies (Thu, 11 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5007534
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Unexpected DNA Affinity and Sequence Selectivity through Core Rigidity in Guanidinium-Based Minor Groove Binders (Thu, 11 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5008006
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Design, Synthesis, and Evaluation of Nonretinoid Retinol Binding Protein 4 Antagonists for the Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease (Thu, 11 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5010013
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Transition State Mimetics of the Plasmodium Export Element Are Potent Inhibitors of Plasmepsin V from P. falciparum and P. vivax (Thu, 11 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500797g
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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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Discovery of 5-Chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an Antidiabetic Clinical Candidate Targeting GPR119 (Wed, 10 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501175v
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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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Identification of a Nonbasic Melanin Hormone Receptor 1 Antagonist as an Antiobesity Clinical Candidate (Tue, 09 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500026w
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Discovery of Novel Highly Potent Hepatitis C Virus NS5A Inhibitor (AV4025) (Tue, 09 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500951r
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Exploring Human Parainfluenza Virus Type-1 Hemagglutinin–Neuraminidase as a Target for Inhibitor Discovery (Mon, 08 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500759v
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Small-Molecule Inhibitors of 25-Hydroxyvitamin D-24-Hydroxylase (CYP24A1): Synthesis and Biological Evaluation (Mon, 08 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5009314
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Potent 11β-Hydroxylase Inhibitors with Inverse Metabolic Stability in Human Plasma and Hepatic S9 Fractions To Promote Wound Healing (Mon, 08 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501004t
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The Design and Synthesis of Potent and Selective Inhibitors of Trypanosoma brucei Glycogen Synthase Kinase 3 for the Treatment of Human African Trypanosomiasis (Mon, 08 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500239b
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Modification on Ursodeoxycholic Acid (UDCA) Scaffold. Discovery of Bile Acid Derivatives As Selective Agonists of Cell-Surface G-Protein Coupled Bile Acid Receptor 1 (GP-BAR1) (Sun, 07 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500889f
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Promiscuity and Selectivity in Covalent Enzyme Inhibition: A Systematic Study of Electrophilic Fragments (Fri, 05 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5006918
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Structure–Activity Relationship of 3,5-Diaryl-2-aminopyridine ALK2 Inhibitors Reveals Unaltered Binding Affinity for Fibrodysplasia Ossificans Progressiva Causing Mutants (Thu, 04 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501177w
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Structure-Based Optimization of a Peptidyl Inhibitor against Calcineurin-Nuclear Factor of Activated T Cell (NFAT) Interaction (Thu, 04 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500743t
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Diarylureas as Allosteric Modulators of the Cannabinoid CB1 Receptor: Structure–Activity Relationship Studies on 1-(4-Chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1) (Thu, 04 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501042u
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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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Development of a Highly Potent, Novel M5 Positive Allosteric Modulator (PAM) Demonstrating CNS Exposure: 1-((1H-Indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380) (Wed, 03 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500995y
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Inhibition of Group IVA Cytosolic Phospholipase A2 by Thiazolyl Ketones in Vitro, ex Vivo, and in Vivo (Wed, 03 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500192s
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Discovery of the CCR1 Antagonist, BMS-817399, for the Treatment of Rheumatoid Arthritis (Wed, 03 Sep 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5003167
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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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Rational Use of Plasma Protein and Tissue Binding Data in Drug Design (Wed, 06 Aug 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5007935
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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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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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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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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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