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.

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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



Nucleoside Derived Antibiotics to Fight Microbial Drug Resistance: New Utilities for an Established Class of Drugs?

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00325

Datum: 27.09.2016


Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01071

Datum: 27.09.2016


Identification of Ligand Binding Hot Spots of the Histamine H1 Receptor following Structure-Based Fragment Optimization

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00981

Datum: 27.09.2016


Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer’s Disease

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00908

Datum: 27.09.2016


Development of Therapeutics That Induce Mitochondrial Biogenesis for the Treatment of Acute and Chronic Degenerative Diseases

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00669

Datum: 27.09.2016


The Rational Design, Synthesis, and Antimicrobial Properties of Thiophene Derivatives That Inhibit Bacterial Histidine Kinases

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00580

Datum: 26.09.2016


Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00420

Datum: 22.09.2016


Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00685

Datum: 22.09.2016


Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00461

Datum: 22.09.2016


Discovery and Optimization of 1-Phenoxy-2-aminoindanes as Potent, Selective, and Orally Bioavailable Inhibitors of the Na+/H+ Exchanger Type 3 (NHE3)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00624

Datum: 22.09.2016


Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00379

Datum: 21.09.2016


Optimization and Structure–Activity Relationships of Phosphinic Pseudotripeptide Inhibitors of Aminopeptidases That Generate Antigenic Peptides

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01031

Datum: 20.09.2016


A Lipophilic Pt(IV) Oxaliplatin Derivative Enhances Antitumor Activity

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00955

Datum: 20.09.2016


Enabling Efficient Positron Emission Tomography (PET) Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) with a Robust and One-Step Radiosynthesis of a Highly Potent 18F-Labeled Ligand ([18F]UCB-H)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00905

Datum: 20.09.2016


Amending HIV Drugs: A Novel Small-Molecule Approach To Target Lupus Anti-DNA Antibodies

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00694

Datum: 20.09.2016


Discovery of Benzothiazole Scaffold-Based DNA Gyrase B Inhibitors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00864

Datum: 20.09.2016


Structure–Activity Relationships and Kinetic Studies of Peptidic Antagonists of CBX Chromodomains

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00801

Datum: 19.09.2016


Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00442

Datum: 19.09.2016


Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01088

Datum: 19.09.2016


Synthesis and Enantiomeric Separation of a Novel Spiroketal Derivative: A Potent Human Telomerase Inhibitor with High in Vitro Anticancer Activity

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01046

Datum: 19.09.2016


Modeling, Synthesis, and Biological Evaluation of Potential Retinoid X Receptor (RXR)-Selective Agonists: Analogues of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and 6-(Ethyl(5,5,8,8-tetrahydronaphthalen-2-yl)amino)nicotinic Acid (NEt-TMN)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00812

Datum: 19.09.2016


β-Sulfonamido Functionalized Aspartate Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype Selectivity Profiles Arising from Subtle Structural Differences

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01066

Datum: 16.09.2016


Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00676

Datum: 15.09.2016


Truncated Autoinducing Peptides as Antagonists of Staphylococcus lugdunensis Quorum Sensing

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00727

Datum: 15.09.2016


Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01033

Datum: 15.09.2016


Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure–Activity Relationship Study

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01058

Datum: 14.09.2016


Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00995

Datum: 12.09.2016


Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00723

Datum: 10.09.2016


Nucleoside Phosphate and Phosphonate Prodrug Clinical Candidates

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00523

Datum: 08.09.2016


Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00438

Datum: 07.09.2016


Driving Structure-Based Drug Discovery through Cosolvent Molecular Dynamics

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00399

Datum: 17.08.2016


Small Molecules in Development for the Treatment of Spinal Muscular Atrophy

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00670

Datum: 16.08.2016


Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00618

Datum: 03.08.2016


Drug-like Antagonists of P2Y ReceptorsFrom Lead Identification to Drug Development

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.5b01972

Datum: 01.08.2016


Transient Receptor Potential Melastatin 8 Channel (TRPM8) Modulation: Cool Entryway for Treating Pain and Cancer

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00305

Datum: 01.08.2016


Therapeutic Potential of Foldamers: From Chemical Biology Tools To Drug Candidates?

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00376

Datum: 29.07.2016


The Medicinal Chemistry of Therapeutic Oligonucleotides

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00551

Datum: 29.07.2016


An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00055

Datum: 27.07.2016


Peptidyl-Proline Isomerases (PPIases): Targets for Natural Products and Natural Product-Inspired Compounds

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00411

Datum: 25.07.2016


Targeting the Translesion Synthesis Pathway for the Development of Anti-Cancer Chemotherapeutics

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00596

Datum: 19.07.2016


Underexplored Opportunities for Natural Products in Drug Discovery

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00473

Datum: 11.07.2016


G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.5b01939

Datum: 08.07.2016


The “Cyclopropyl Fragment” is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00472

Datum: 30.06.2016


Blocking Blood Flow to Solid Tumors by Destabilizing Tubulin: An Approach to Targeting Tumor Growth

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00463

Datum: 27.06.2016


Metabolomics as a Challenging Approach for Medicinal Chemistry and Personalized Medicine

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.5b01335

Datum: 27.06.2016


Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b00150

Datum: 03.06.2016






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