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Journal of Medicinal Chemistry

Current research reports and chronological list of recent articles..




The international scientific Journal of Medicinal Chemistry publishes studies that contribute to an understanding of the relationship between molecular structure and biological activity or mode of action.

The publisher is the American Chemical Society, ACS. The copyright and publishing rights of specialized products listed below are in this publishing house. This is also responsible for the content shown.

To search this web page for specific words type "Ctrl" + "F" on your keyboard (Command + "F" on a Mac). Then: type the word you are searching for in the window that pops up!

Additional research articles see Current Chemistry Research Articles. Magazines with similar content (medicinal chemistry):

 - Bioorganic and Medicinal Chemistry Letters,

 - European Journal of Medicinal Chemistry,

 - Journal of Enzyme Inhibition and Medicinal Chemistry,

 - Medicinal Chemistry Research.



Journal of Medicinal Chemistry - Abstracts



Tozasertib Analogues as Inhibitors of Necroptotic Cell Death

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01449

Datum: 20.02.2018


Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01690

Datum: 16.02.2018


Glutathione S-Transferase π-Activatable O2-(Sulfonylethyl Derived) Diazeniumdiolates Potently Suppress Melanoma in Vitro and in Vivo

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01178

Datum: 16.02.2018


Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline–Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer’s Disease

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01417

Datum: 15.02.2018


Design and Syntheses of Highly Potent Teixobactin Analogues against Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), and Vancomycin-Resistant Enterococci (VRE) in Vitro and in Vivo

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01634

Datum: 15.02.2018


Identification and Mitigation of Reactive Metabolites of 2-Aminoimidazole-Containing Microsomal Prostaglandin E Synthase-1 Inhibitors Terminated Due to Clinical Drug-Induced Liver Injury

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01806

Datum: 15.02.2018


Synthesis and Bioactivity Investigation of the Individual Components of Cyclic Lipopeptide Antibiotics

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01367

Datum: 15.02.2018


Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro-N-acetylneuraminic Acid Derivatives

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01467

Datum: 15.02.2018


Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01096

Datum: 15.02.2018


Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01438

Datum: 14.02.2018


Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01314

Datum: 14.02.2018


The Synthesized Plant Metabolite 3,4,5-Tri-O-Galloylquinic Acid Methyl Ester Inhibits Calcium Oxalate Crystal Growth in a Drosophila Model, Downregulates Renal Cell Surface Annexin A1 Expression, and Decreases Crystal Adhesion to Cells

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01566

Datum: 13.02.2018


Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01858

Datum: 12.02.2018


Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01261

Datum: 12.02.2018


Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure–Activity and Structure–Property Relationship Studies

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00738

Datum: 09.02.2018


Allosteric Modulators of Drug Targets Special Issue

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00171

Datum: 07.02.2018


Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01895

Datum: 07.02.2018


Targeting Multiple Effector Pathways in Pancreatic Ductal Adenocarcinoma with a G-Quadruplex-Binding Small Molecule

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01781

Datum: 07.02.2018


A Dual Reporter Iodinated Labeling Reagent for Cancer Positron Emission Tomography Imaging and Fluorescence-Guided Surgery

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01746

Datum: 06.02.2018


New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01710

Datum: 06.02.2018


Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01765

Datum: 06.02.2018


Salutaxel, a Conjugate of Docetaxel and a Muramyl Dipeptide (MDP) Analogue, Acts as Multifunctional Prodrug That Inhibits Tumor Growth and Metastasis

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01407

Datum: 06.02.2018


Synthesis and Pharmacological Characterization of C4β-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1S,2S,4S,5R,6S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu3 Receptor Agonist

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01481

Datum: 06.02.2018


Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01465

Datum: 06.02.2018


Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01788

Datum: 05.02.2018


Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer’s Disease

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01370

Datum: 05.02.2018


Structure–Activity Relationships and Computational Investigations into the Development of Potent and Balanced Dual-Acting Butyrylcholinesterase Inhibitors and Human Cannabinoid Receptor 2 Ligands with Pro-Cognitive in Vivo Profiles

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01760

Datum: 05.02.2018


The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01731

Datum: 05.02.2018


The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaV1.6

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01609

Datum: 03.02.2018


Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01153

Datum: 02.02.2018


Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01769

Datum: 02.02.2018


Design and Synthesis of Novel Reactive Oxygen Species Inducers for the Treatment of Pancreatic Ductal Adenocarcinoma

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01463

Datum: 02.02.2018


Progress in the Development of Preventative Drugs for Cisplatin-Induced Hearing Loss

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01653

Datum: 01.02.2018


Interfering with HuR–RNA Interaction: Design, Synthesis and Biological Characterization of Tanshinone Mimics as Novel, Effective HuR Inhibitors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01176

Datum: 31.01.2018


Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01422

Datum: 31.01.2018


Synthesis and Structure–Activity Relationship (SAR) Studies of Novel Pyrazolopyridine Derivatives as Inhibitors of Enterovirus Replication

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01863

Datum: 31.01.2018


Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00925

Datum: 19.01.2018


Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00873

Datum: 17.01.2018


Emerging New Targets for the Treatment of Resistant Fungal Infections

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01413

Datum: 16.01.2018


Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01288

Datum: 10.01.2018


Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00901

Datum: 09.01.2018


High Mobility Group Box-1 (HMGb1): Current Wisdom and Advancement as a Potential Drug Target

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01136

Datum: 05.01.2018


Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01607

Datum: 05.01.2018


Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01339

Datum: 05.01.2018


Targeting Transcriptional Enhanced Associate Domains (TEADs)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00879

Datum: 28.12.2017


Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01457

Datum: 28.12.2017


The Rise and Fall of a Scaffold: A Trend Analysis of Scaffolds in the Medicinal Chemistry Literature

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00954

Datum: 27.12.2017


Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01019

Datum: 20.12.2017


Small Molecule Mitochondrial Uncouplers and Their Therapeutic Potential

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01182

Datum: 08.12.2017


Importance of Rigidity in Designing Small Molecule Drugs To Tackle Protein–Protein Interactions (PPIs) through Stabilization of Desired Conformers

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01120

Datum: 28.11.2017


Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01310

Datum: 27.11.2017


Relevance of Half-Life in Drug Design

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00969

Datum: 17.11.2017


Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00772

Datum: 09.11.2017


Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00718

Datum: 01.11.2017


Fragment-to-Lead Medicinal Chemistry Publications in 2016

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01298

Datum: 31.10.2017


Modulators of 14-3-3 Protein–Protein Interactions

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00574

Datum: 19.10.2017


Chemical Approaches to Modulating Complement-Mediated Diseases

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00882

Datum: 18.10.2017


Learning Medicinal Chemistry Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Rules from Cross-Company Matched Molecular Pairs Analysis (MMPA)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00935

Datum: 28.09.2017


Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00717

Datum: 27.09.2017


Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00956

Datum: 22.09.2017


Carbon Monoxide and Its Controlled Release: Therapeutic Application, Detection, and Development of Carbon Monoxide Releasing Molecules (CORMs)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01153

Datum: 20.09.2017


Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00315

Datum: 08.09.2017


Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01827

Datum: 25.08.2017


The ProTide Prodrug Technology: From the Concept to the Clinic

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00734

Datum: 24.08.2017


Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00115

Datum: 22.08.2017


Causes and Significance of Increased Compound Potency in Cellular or Physiological Contexts

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00762

Datum: 18.08.2017


Fragment-Based Drug Discovery of Phosphodiesterase Inhibitors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00404

Datum: 11.08.2017


The Current State of Peptide Drug Discovery: Back to the Future?

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00318

Datum: 11.08.2017


Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01817

Datum: 24.05.2017


 


Category: Current Chemistry Research

Last update: 04.01.2018.






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