Journal of Medicinal Chemistry

Discovery of 1,2,3-Triazole Derivatives for Multimodality PET/CT/Cryoimaging of Myelination in the Central Nervous System (Fri, 20 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01328
>> read more

Development of the First Two-Pore Domain Potassium Channel TWIK-Related K+ Channel 1-Selective Agonist Possessing in Vivo Antinociceptive Activity (Fri, 20 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01285
>> read more

Total Syntheses and Biological Activities of Vinylamycin Analogues (Fri, 20 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01745
>> read more

Antileishmanial Activity of Pyrazolopyridine Derivatives and Their Potential as an Adjunct Therapy with Miltefosine (Fri, 20 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01447
>> read more

Peptide Macrocycle Inhibitor of Coagulation Factor XII with Subnanomolar Affinity and High Target Selectivity (Fri, 20 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01548
>> read more

Pyrimidinyl Biphenylureas: Identification of New Lead Compounds as Allosteric Modulators of the Cannabinoid Receptor CB1 (Thu, 19 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01448
>> read more

Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension (Thu, 19 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00871
>> read more

Design, Synthesis, and Biological Evaluation of Small, High-Affinity Siglec-7 Ligands: Toward Novel Inhibitors of Cancer Immune Evasion (Thu, 19 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01111
>> read more

Potent Inhibition of Nitric Oxide-Releasing Bifendate Derivatives against Drug-Resistant K562/A02 Cells in Vitro and in Vivo (Wed, 18 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01075
>> read more

Structure–Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439) (Wed, 18 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01586
>> read more

Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies (Wed, 18 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01418
>> read more

Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold (Wed, 18 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01509
>> read more

Targeting Type 2 Diabetes with C-Glucosyl Dihydrochalcones as Selective Sodium Glucose Co-Transporter 2 (SGLT2) Inhibitors: Synthesis and Biological Evaluation (Wed, 18 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01134
>> read more

A Macrocyclic Agouti-Related Protein/[Nle4,DPhe7]α-Melanocyte Stimulating Hormone Chimeric Scaffold Produces Subnanomolar Melanocortin Receptor Ligands (Tue, 17 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01707
>> read more

Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A2A Receptor Antagonists and Their Biological Evaluation (Tue, 17 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01584
>> read more

Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3 (Tue, 17 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01180
>> read more

Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes (Tue, 17 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01541
>> read more

Difluoromethyl Bioisostere: Examining the “Lipophilic Hydrogen Bond Donor” Concept (Tue, 17 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01691
>> read more

N-Heterocyclic (4-Phenylpiperazin-1-yl)methanones Derived from Phenoxazine and Phenothiazine as Highly Potent Inhibitors of Tubulin Polymerization (Fri, 13 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01591
>> read more

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K) (Thu, 12 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01363
>> read more

The Essential Medicinal Chemistry of Curcumin (Wed, 11 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00975
>> read more

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies (Mon, 09 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01583
>> read more

Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity (Mon, 09 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01574
>> read more

Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach (Mon, 09 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01007
>> read more

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe (Mon, 09 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01566
>> read more

Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein–Protein Interaction Inhibitors Targeting the EphA2 Receptor (Thu, 05 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01642
>> read more

Structure–Activity Relationships of Small Molecule Autotaxin Inhibitors with a Discrete Binding Mode (Thu, 05 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01597
>> read more

Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome (Thu, 05 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01196
>> read more

Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics (Thu, 05 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01474
>> read more

Toward Understanding the Structural Basis of Partial Agonism at the Dopamine D3 Receptor (Thu, 05 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01148
>> read more

Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin (Wed, 04 Jan 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01634
>> read more

Combining Molecular Scaffolds from FDA Approved Drugs: Application to Drug Discovery (Fri, 23 Dec 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01367
>> read more

Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy (Thu, 22 Dec 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01167
>> read more

The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors (Wed, 21 Dec 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01496
>> read more

Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors (Wed, 21 Dec 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00990
>> read more

Recent Advances in Scaffold Hopping (Wed, 21 Dec 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01437
>> read more

Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions (Tue, 20 Dec 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00788
>> read more

Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis (Mon, 19 Dec 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01163
>> read more

Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules (Tue, 13 Dec 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b01888
>> read more

Idiopathic Pulmonary Fibrosis: Current Status, Recent Progress, and Emerging Targets (Tue, 29 Nov 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b00935
>> read more

Recent Progress in the Development of Transglutaminase 2 (TGase2) Inhibitors (Mon, 21 Nov 2016)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01036
>> read more

Site Search