Journal of Medicinal Chemistry

The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits (Thu, 02 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00313
>> read more

Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton’s Tyrosine Kinase (Thu, 02 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00734
>> read more

18F-Labeled 1,4-Dioxa-8-azaspiro[4.5]decane Derivative: Synthesis and Biological Evaluation of a σ1 Receptor Radioligand with Low Lipophilicity as Potent Tumor Imaging Agent (Thu, 02 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00593
>> read more

Therapeutic Potential of 5-HT6 Receptor Agonists (Thu, 02 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00179
>> read more

Development of 2-Deoxy-2-[18F]fluororibose for Positron Emission Tomography Imaging Liver Function in Vivo (Thu, 02 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00569
>> read more

Peptidomimetic β-Secretase Inhibitors Comprising a Sequence of Amyloid-β Peptide for Alzheimer’s Disease (Wed, 01 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00658
>> read more

Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators (Wed, 01 Jul 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00229
>> read more

Correction to Deciphering the Mechanism of Carbonic Anhydrase Inhibition with Coumarins and Thiocoumarins (Tue, 30 Jun 2015)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00969
>> read more

Potent Apoptotic Response Induced by Chloroacetamidine Anthrathiophenediones in Bladder Cancer Cells (Tue, 30 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00409
>> read more

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH) (Tue, 30 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00606
>> read more

Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223 (Fri, 26 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00626
>> read more

Synthesis of Piperlongumine Analogues and Discovery of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators as Potential Neuroprotective Agents (Fri, 26 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00410
>> read more

Aurora Kinase Inhibition: A New Light in the Sky? (Thu, 25 Jun 2015)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00918
>> read more

Fragment-Based Exploration of Binding Site Flexibility in Mycobacterium tuberculosis BioA (Wed, 24 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00092
>> read more

Structure-Based Design of Potent HIV-1 Protease Inhibitors with Modified P1-Biphenyl Ligands: Synthesis, Biological Evaluation, and Enzyme–Inhibitor X-ray Structural Studies (Wed, 24 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00676
>> read more

Structure–Activity Study of N-((trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a Bitopic Ligand That Acts as a Negative Allosteric Modulator of the Dopamine D2 Receptor (Wed, 24 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00581
>> read more

A Selective Prostaglandin E2 Receptor Subtype 2 (EP2) Antagonist Increases the Macrophage-Mediated Clearance of Amyloid-Beta Plaques (Wed, 24 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00567
>> read more

Antiangiogenic Activity of Mononuclear Copper(II) Polypyridyl Complexes for the Treatment of Cancers (Wed, 24 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00651
>> read more

Discovery of 1-{4-[3-Fluoro-4-((3S,6R)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist (Tue, 23 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00597
>> read more

Design, Synthesis, and Anticonvulsant Activity of New Hybrid Compounds Derived from 2-(2,5-Dioxopyrrolidin-1-yl)propanamides and 2-(2,5-Dioxopyrrolidin-1-yl)butanamides (Tue, 23 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00578
>> read more

Benzoxaborole Antimalarial Agents. Part 4. Discovery of Potent 6-(2-(Alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles (Tue, 23 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00678
>> read more

Development of Novel CXC Chemokine Receptor 7 (CXCR7) Ligands: Selectivity Switch from CXCR4 Antagonists with a Cyclic Pentapeptide Scaffold (Thu, 18 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00216
>> read more

One-Pot Reaction To Obtain N,N′-Disubstituted Guanidines of Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine Scaffold as Human A3 Adenosine Receptor Antagonists (Wed, 17 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00551
>> read more

Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women’s Health (Fri, 12 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00386
>> read more

Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators (Wed, 03 Jun 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00516
>> read more

Discovery of N-(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines (Sun, 31 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00183
>> read more

Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors (Tue, 26 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00326
>> read more

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF (Wed, 20 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00458
>> read more

Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications (Thu, 14 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501981g
>> read more

Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors (Thu, 14 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00261
>> read more

New Frontiers in Selective Human MAO-B Inhibitors (Mon, 11 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501690r
>> read more

Ligand Binding Thermodynamics in Drug Discovery: Still a Hot Tip? (Mon, 11 May 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501511f
>> read more

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition (Thu, 30 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00256
>> read more

Activation of the γ-Aminobutyric Acid Type B (GABAB) Receptor by Agonists and Positive Allosteric Modulators (Fri, 24 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5018913
>> read more

Progress Toward the Development of Noscapine and Derivatives as Anticancer Agents (Thu, 16 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501180v
>> read more

Peroxisome Proliferator-Activated Receptor γ (PPARγ) and Ligand Choreography: Newcomers Take the Stage (Thu, 09 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501155f
>> read more

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B (Mon, 06 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00209
>> read more

Volume of Distribution in Drug Design (Wed, 01 Apr 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00201
>> read more

Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis (Tue, 31 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501512b
>> read more

Clostridium difficile Drug Pipeline: Challenges in Discovery and Development of New Agents (Mon, 30 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5016846
>> read more

Fighting Malaria: Structure-Guided Discovery of Nonpeptidomimetic Plasmepsin Inhibitors (Tue, 17 Mar 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5014133
>> read more

Site Search