Journal of Medicinal Chemistry

4-Alkyloxyimino Derivatives of Uridine-5′-triphosphate: Distal Modification of Potent Agonists as a Strategy for Molecular Probes of P2Y2, P2Y4, and P2Y6 Receptors (Fri, 18 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500367e
>> read more

Discovery, Synthesis, and Optimization of Antimalarial 4(1H)-Quinolone-3-Diarylethers (Fri, 18 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500147k
>> read more

Indirubin Core Structure of Glycogen Synthase Kinase-3 Inhibitors as Novel Chemotype for Intervention with 5-Lipoxygenase (Thu, 17 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401740w
>> read more

Motor Neuron Disease: A Chemical Perspective (Thu, 17 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5001584
>> read more

Diacylglycerol Lactones Targeting the Structural Features That Distinguish the Atypical C1 Domains of Protein Kinase C ζ and ι from Typical C1 Domains (Thu, 17 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500165n
>> read more

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
>> read more

New Potent Antibacterial Oxazolidinone (MRX-I) with an Improved Class Safety Profile (Wed, 16 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401931e
>> read more

Matched Molecular Pair Analysis: Significance and the Impact of Experimental Uncertainty (Wed, 16 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500317a
>> read more

Discovery of a Neuroprotective Chemical, (S)-N-(3-(3,6-Dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(−)-P7C3-S243], with Improved Druglike Properties (Wed, 16 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401919s
>> read more

Thermodynamic and Structural Characterization of Halogen Bonding in Protein–Ligand Interactions: A Case Study of PDE5 and Its Inhibitors (Tue, 15 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5002315
>> read more

Exploring the Water-Binding Pocket of the Type II Dehydroquinase Enzyme in the Structure-Based Design of Inhibitors (Tue, 15 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500175z
>> read more

Birinapant, a Smac-Mimetic with Improved Tolerability for the Treatment of Solid Tumors and Hematological Malignancies (Tue, 15 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500176w
>> read more

Bis-alkylamine Indolo[3,2-b]quinolines as Hemozoin Ligands: Implications for Antimalarial Cytostatic and Cytocidal Activities (Tue, 15 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500075d
>> read more

Development of Pyrazolone and Isoxazol-5-one Cambinol Analogues as Sirtuin Inhibitors (Tue, 15 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4018064
>> read more

Identification and Characterization of Small Molecule Modulators of the Epstein–Barr Virus-Induced Gene 2 (EBI2) Receptor (Tue, 15 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4019355
>> read more

Discovery of the First N-Hydroxycinnamamide-Based Histone Deacetylase 1/3 Dual Inhibitors with Potent Oral Antitumor Activity (Tue, 15 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401877m
>> read more

Far-Red Light Activatable, Multifunctional Prodrug for Fluorescence Optical Imaging and Combinational Treatment (Mon, 14 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5000722
>> read more

Novel Derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with Improved Fluorescent and σ Receptors Binding Properties (Mon, 14 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401874n
>> read more

Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase (Fri, 11 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5001503
>> read more

Cyclic Secondary Sulfonamides: Unusually Good Inhibitors of Cancer-Related Carbonic Anhydrase Enzymes (Fri, 11 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500255y
>> read more

Optimization of an Imidazopyridazine Series of Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 (PfCDPK1) (Fri, 11 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500342d
>> read more

Discovery of a Novel Series of Orally Active Nociceptin/Orphanin FQ (NOP) Receptor Antagonists Based on a Dihydrospiro(piperidine-4,7′-thieno[2,3-c]pyran) Scaffold (Fri, 11 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500117r
>> read more

Discovery, Optimization, and Characterization of Novel D2 Dopamine Receptor Selective Antagonists (Thu, 10 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500126s
>> read more

Identification of Novel HSP90α/β Isoform Selective Inhibitors Using Structure-Based Drug Design. Demonstration of Potential Utility in Treating CNS Disorders such as Huntington’s Disease (Thu, 10 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500042s
>> read more

Discovery of Selective 4-Amino-pyridopyrimidine Inhibitors of MAP4K4 Using Fragment-Based Lead Identification and Optimization (Wed, 09 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500155b
>> read more

Thienoquinolines as Novel Disruptors of the PKCε/RACK2 Protein–Protein Interaction (Tue, 08 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401605c
>> read more

Discovery of 6-Phenylpyrimido[4,5-b][1,4]oxazines as Potent and Selective Acyl CoA:Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors with in Vivo Efficacy in Rodents (Tue, 08 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500135c
>> read more

Pharmacophoric Modifications Lead to Superpotent αvβ3 Integrin Ligands with Suppressed α5β1 Activity (Tue, 08 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500092w
>> read more

Discovery of 2-[3,5-Dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β Agonist in Clinical Trials for the Treatment of Dyslipidemia (Tue, 08 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4019299
>> read more

Allosteric Inhibition of Human Factor XIa: Discovery of Monosulfated Benzofurans as a Class of Promising Inhibitors (Mon, 07 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5002698
>> read more

Triaryl-Substituted Schiff Bases Are High-Affinity Subtype-Selective Ligands for the Estrogen Receptor (Mon, 07 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500268j
>> read more

Design, Synthesis, and Biological Evaluation of Novel Pyridine-Bridged Analogues of Combretastatin-A4 as Anticancer Agents (Mon, 07 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500002k
>> read more

Discovery of Trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as Potent, Orally Bioavailable TGR5 (GPBAR1) Agonists: Structure–Activity Relationships, Lead Optimization, and Chronic In Vivo Efficacy (Fri, 04 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401731q
>> read more

Agonists for the Adenosine A1 Receptor with Tunable Residence Time. A Case for Nonribose 4-Amino-6-aryl-5-cyano-2-thiopyrimidines (Thu, 03 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401643m
>> read more

Discovery of a Potent and Selective α3β4 Nicotinic Acetylcholine Receptor Antagonist from an α-Conotoxin Synthetic Combinatorial Library (Thu, 03 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500183r
>> read more

Discovery of a Highly Tumor-Selective Organometallic Ruthenium(II)–Arene Complex (Wed, 02 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5002748
>> read more

Discovery of AMG 925, a FLT3 and CDK4 Dual Kinase Inhibitor with Preferential Affinity for the Activated State of FLT3 (Wed, 02 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500118j
>> read more

Synthesis, Structure–Activity Relationships, and Biological Studies of Chromenochalcones as Potential Antileishmanial Agents (Wed, 02 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401893j
>> read more

Omarigliptin (MK-3102): A Novel Long-Acting DPP-4 Inhibitor for Once-Weekly Treatment of Type 2 Diabetes (Wed, 02 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401992e
>> read more

New Pyrazolobenzothiazine Derivatives as Hepatitis C Virus NS5B Polymerase Palm Site I Inhibitors (Wed, 02 Apr 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401688h
>> read more

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
>> read more

Design, Synthesis, and Structure–Activity Relationship Studies of Novel Fused Heterocycles-Linked Triazoles with Good Activity and Water Solubility (Fri, 07 Mar 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4016284
>> read more

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
>> read more

Hydrocarbon-Stapled Peptides: Principles, Practice, and Progress (Thu, 06 Mar 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4011675
>> read more

The Current State of Drug Discovery and a Potential Role for NMR Metabolomics (Mon, 03 Mar 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401803b
>> read more

Therapeutic Melting Pot of Never in Mitosis Gene A Related Kinase 2 (Nek2): A Perspective on Nek2 as an Oncology Target and Recent Advancements in Nek2 Small Molecule Inhibition (Tue, 25 Feb 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401719n
>> read more

Modulators of the Nuclear Receptor Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc) (Mon, 24 Feb 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401901d
>> read more

Rings in Drugs (Mon, 17 Feb 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4017625
>> read more

Switching Invariant Natural Killer T (iNKT) Cell Response from Anticancerous to Anti-Inflammatory Effect: Molecular Bases (Wed, 12 Feb 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4010863
>> read more

Importance of Sphingosine Kinase (SphK) as a Target in Developing Cancer Therapeutics and Recent Developments in the Synthesis of Novel SphK Inhibitors (Tue, 11 Feb 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4011687
>> read more

Discovery of Innovative Therapeutics: Today’s Realities and Tomorrow’s Vision. 2. Pharma’s Challenges and Their Commitment to Innovation (Fri, 07 Feb 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401564r
>> read more

Foundation-Directed Therapeutic Development in Huntington’s Disease (Tue, 04 Feb 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4009295
>> read more

Aldosterone Synthase Inhibitors as Promising Treatments for Mineralocorticoid Dependent Cardiovascular and Renal Diseases (Fri, 24 Jan 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401430e
>> read more

Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases (Thu, 23 Jan 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401490p
>> read more

QSAR Modeling: Where Have You Been? Where Are You Going To? (Mon, 06 Jan 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4004285
>> read more

Opportunities and Challenges in Developing Stearoyl-Coenzyme A Desaturase-1 Inhibitors as Novel Therapeutics for Human Disease (Fri, 20 Dec 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401516c
>> read more

Targeting Receptor Tyrosine Kinase MET in Cancer: Small Molecule Inhibitors and Clinical Progress (Wed, 18 Dec 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401427c
>> read more

Medicinal Chemistry of Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) (Fri, 13 Dec 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4014746
>> read more

5-HT1A Receptor: An Old Target as a New Attractive Tool in Drug Discovery from Central Nervous System to Cancer (Tue, 10 Dec 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm400533t
>> read more

Prostanoid Receptor EP2 as a Therapeutic Target (Wed, 04 Dec 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401431x
>> read more

Using Deuterium in Drug Discovery: Leaving the Label in the Drug (Mon, 02 Dec 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4007998
>> read more

Recent Advances in the Discovery of Small Molecules Targeting Exchange Proteins Directly Activated by cAMP (EPAC) (Wed, 27 Nov 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401425e
>> read more

Toll-like Receptor 4 (TLR4) Modulation by Synthetic and Natural Compounds: An Update (Wed, 20 Nov 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401006s
>> read more

Adenosine A2A Receptor as a Drug Discovery Target (Fri, 15 Nov 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm4011669
>> read more

MT1 and MT2 Melatonin Receptors: Ligands, Models, Oligomers, and Therapeutic Potential (Thu, 14 Nov 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401343c
>> read more

Molecular Similarity in Medicinal Chemistry (Mon, 11 Nov 2013)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm401411z
>> read more

Site Search