Journal of Medicinal Chemistry

Exploitation of the Ability of γ-Tocopherol to Facilitate Membrane Co-localization of Akt and PHLPP1 to Develop PHLPP1-Targeted Akt Inhibitors (Fri, 27 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501751b
>> read more

Identification of the Molecular Basis of Inhibitor Selectivity between the Human and Streptococcal Type I Methionine Aminopeptidases (Fri, 27 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501790e
>> read more

5′-C-Ethyl-tetrazolyl-N6-Substituted Adenosine and 2-Chloro-adenosine Derivatives as Highly Potent Dual Acting A1 Adenosine Receptor Agonists and A3 Adenosine Receptor Antagonists (Fri, 27 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00074
>> read more

Correction to Tetra-Substituted Pyridinylimidazoles As Dual Inhibitors of p38α Mitogen-Activated Protein Kinase and c-Jun N-Terminal Kinase 3 for Potential Treatment of Neurodegenerative Diseases (Thu, 26 Feb 2015)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00235
>> read more

Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B (Thu, 26 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501963e
>> read more

Development of a Novel Class of Tubulin Inhibitor from Desmosdumotin B with a Hydroxylated Bicyclic B-Ring (Thu, 26 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501859j
>> read more

Small Molecule Binding Sites on the Ras:SOS Complex Can Be Exploited for Inhibition of Ras Activation (Thu, 26 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501660t
>> read more

A Binding Mode Hypothesis of Tiagabine Confirms Liothyronine Effect on γ-Aminobutyric Acid Transporter 1 (GAT1) (Thu, 26 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5015428
>> read more

Quantum Chemistry Calculation-Aided Structural Optimization of Combretastatin A-4-like Tubulin Polymerization Inhibitors: Improved Stability and Biological Activity (Thu, 26 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00118
>> read more

Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity (Thu, 26 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501258m
>> read more

Structure-Based Lead Optimization and Biological Evaluation of BAX Direct Activators as Novel Potential Anticancer Agents (Wed, 25 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501123r
>> read more

Design and Optimization of a Series of 1-Sulfonylpyrazolo[4,3-b]pyridines as Selective c-Met Inhibitors (Wed, 25 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm502018y
>> read more

Strong Antibacterial Properties of Anion Transporters: A Result of Depolarization and Weakening of the Bacterial Membrane (Wed, 25 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501979f
>> read more

Design, Synthesis, and Biological Evaluation of Novel Matrix Metalloproteinase Inhibitors As Potent Antihemorrhagic Agents: From Hit Identification to an Optimized Lead (Wed, 25 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501940y
>> read more

Discovery and Safety Profiling of a Potent Preclinical Candidate, (4-[4-[[(3R)-3-(Hydroxycarbamoyl)-8-azaspiro[4.5]decan-3-yl]sulfonyl]phenoxy]-N-methylbenzamide) (CM-352), for the Prevention and Treatment of Hemorrhage (Wed, 25 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501939z
>> read more

Tau Positron Emission Tomography (PET) Imaging: Past, Present, and Future (Wed, 25 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5017544
>> read more

Structure Diversification of Vancomycin through Peptide-Catalyzed, Site-Selective Lipidation: A Catalysis-Based Approach To Combat Glycopeptide-Resistant Pathogens (Tue, 24 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501872s
>> read more

Learning from PAINful lessons (Tue, 24 Feb 2015)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00294
>> read more

C-Terminal Modifications of Apelin-13 Significantly Change Ligand Binding, Receptor Signaling, and Hypotensive Action (Tue, 24 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501916k
>> read more

Synthesis of CDDO–Amino Acid–Nitric Oxide Donor Trihybrids as Potential Antitumor Agents against Both Drug-Sensitive and Drug-Resistant Colon Cancer (Mon, 23 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5019302
>> read more

Discovery of Novel 2,5-Dioxoimidazolidine-Based P2X7 Receptor Antagonists as Constrained Analogues of KN62 (Mon, 23 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500324g
>> read more

PAINS in the Assay: Chemical Mechanisms of Assay Interference and Promiscuous Enzymatic Inhibition Observed during a Sulfhydryl-Scavenging HTS (Sat, 21 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5019093
>> read more

Selective, Nontoxic CB2 Cannabinoid o-Quinone with in Vivo Activity against Triple-Negative Breast Cancer (Fri, 20 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.5b00078
>> read more

Activity of 2-Aryl-2-(3-indolyl)acetohydroxamates against Drug-Resistant Cancer Cells (Fri, 20 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501518y
>> read more

Synthetic Nucleic Acid Delivery Systems: Present and Perspectives (Fri, 20 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500330k
>> read more

FimH Antagonists: Bioisosteres To Improve the in Vitro and in Vivo PK/PD Profile (Fri, 20 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501524q
>> read more

Synthesis and Structure–Activity Relationship Study of a New Series of Selective σ1 Receptor Ligands for the Treatment of Pain: 4-Aminotriazoles (Thu, 19 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501920g
>> read more

Understanding Our Love Affair with p-Chlorophenyl: Present Day Implications from Historical Biases of Reagent Selection (Thu, 19 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501894t
>> read more

Engineering Potent and Selective Analogues of GpTx-1, a Tarantula Venom Peptide Antagonist of the NaV1.7 Sodium Channel (Thu, 19 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501765v
>> read more

Synthesis and Biological Evaluation of Indolyl-Pyridinyl-Propenones Having Either Methuosis or Microtubule Disruption Activity (Thu, 19 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501997q
>> read more

Discovery of AZD3147: A Potent, Selective Dual Inhibitor of mTORC1 and mTORC2 (Wed, 18 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501778s
>> read more

Discovery of Highly Selective Brain-Penetrant Vasopressin 1a Antagonists for the Potential Treatment of Autism via a Chemogenomic and Scaffold Hopping Approach (Wed, 18 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501745f
>> read more

Stabilization of G-Quadruplex DNA, Inhibition of Telomerase Activity, and Tumor Cell Apoptosis by Organoplatinum(II) Complexes with Oxoisoaporphine (Wed, 18 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5012484
>> read more

Design, Synthesis, and Biological Evaluation of Theranostic Vitamin–Linker–Taxoid Conjugates (Wed, 18 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5019115
>> read more

Selective Nonpeptidic Fluorescent Ligands for Oxytocin Receptor: Design, Synthesis, and Application to Time-Resolved FRET Binding Assay (Thu, 12 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501395b
>> read more

Discovery of (R)-1-(3-((2-Chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1′-Biphenyl]-2-ylcarbamate (TD-5959, GSK961081, Batefenterol): First-in-Class Dual Pharmacology Multivalent Muscarinic Antagonist and β2 Agonist (MABA) for the Treatment of Chronic Obstructive Pulmonary Disease (COPD) (Mon, 09 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501915g
>> read more

Bronchodilating Drugs for Chronic Obstructive Pulmonary Disease: Current Status and Future Trends (Mon, 09 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5013227
>> read more

Antitumor Sulfonylhydrazines: Design, Structure–Activity Relationships, Resistance Mechanisms, and Strategies for Improving Therapeutic Utility (Mon, 09 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501459c
>> read more

Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer (Wed, 04 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501464c
>> read more

(Dis)similar Analogues of Riboswitch Metabolites as Antibacterial Lead Compounds (Tue, 03 Feb 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500868e
>> read more

Discovery and Development of Galeterone (TOK-001 or VN/124-1) for the Treatment of All Stages of Prostate Cancer (Wed, 28 Jan 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501239f
>> read more

Small Molecule Discoidin Domain Receptor Kinase Inhibitors and Potential Medical Applications (Wed, 21 Jan 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5012319
>> read more

Stemistry: The Control of Stem Cells in Situ Using Chemistry (Thu, 15 Jan 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500838d
>> read more

Organic Carbamates in Drug Design and Medicinal Chemistry (Wed, 07 Jan 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501371s
>> read more

CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure (Tue, 06 Jan 2015)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm501535r
>> read more

Targeting DNA Methylation with Small Molecules: What’s Next? (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500843d
>> read more

Parallel Worlds of Public and Commercial Bioactive Chemistry Data (Thu, 04 Dec 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm5011308
>> read more

Targeting Aldose Reductase for the Treatment of Diabetes Complications and Inflammatory Diseases: New Insights and Future Directions (Mon, 17 Nov 2014)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/jm500907a
>> read more

Site Search