Cover image for Vol. 10 Issue 8

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 2.968

ISI Journal Citation Reports © Ranking: 2014: 19/59 (Chemistry Medicinal); 83/254 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

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July 28, 2015

Metalloprotein Inhibitors Session, August 17, 2015 ACS National Meeting, Boston

Metalloprotein Inhibitors Session, August 17, 2015 ACS National Meeting, BostonChemMedChem International Advisory Board member Seth Cohen (UC San Diego) and Zachary Sweeney (Denali Therapeutics) will be chairing a session at the 250th American Chemical Society National Meeting & Exposition (Boston, USA) entitled Metalloprotein Inhibitors: Drugs, Drug Candidates, and New Targets at the Interface of Medicinal and Inorganic Chemistry. Among the speakers are ChemMedChem authors Christopher Schofield (University of Oxford), Abbas Walji (Merck Co. Inc.), and of course, Seth Cohen. The session will take place on Monday August 17th from 1:30PM to 5:20PM in Room 160C of the Boston Convention & Exhibition Center. Read more...

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Recently Published Articles

  1. Application of MS Transport Assays to the Four Human γ-Aminobutyric Acid Transporters

    Dr. Sebastian Schmitt, Dr. Georg Höfner and Prof. Dr. Klaus T. Wanner

    Article first published online: 27 JUL 2015 | DOI: 10.1002/cmdc.201500254

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    MS Transport Assays: We describe the application of mass spectrometry based MS Transport Assays toward all four human γ-aminobutyric acid (GABA) transporters. Data for several inhibitors are presented and compared with state-of-the-art radiometric uptake assays. Moreover, a method to evaluate the inhibition curves by taking nonspecific transport into account is discussed in detail.

  2. Perspectives on Inhibiting β-Amyloid Aggregation through Structure-Based Drug Design

    Pankaj Mishra, Dr. Senthil R. Ayyannan and Dr. Gautam Panda

    Article first published online: 24 JUL 2015 | DOI: 10.1002/cmdc.201500215

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    New horizons in biospace: Although the utility of structure-based drug design principles in devising ways to inhibit β-amyloid aggregation with small molecules is still in its early stages, there are unexplored avenues that can be taken in this regard. Herein we discuss the current state of the art in this field of developing drugs to combat Alzheimer′s disease.

  3. Synthesis and Antiplasmodial Activity of Novel Chloroquine Analogues with Bulky Basic Side Chains

    Dr. Bruno Tasso, Dr. Federica Novelli, Dr. Michele Tonelli, Dr. Anna Barteselli, Dr. Nicoletta Basilico, Dr. Silvia Parapini, Prof. Donatella Taramelli, Prof. Anna Sparatore and Prof. Fabio Sparatore

    Article first published online: 24 JUL 2015 | DOI: 10.1002/cmdc.201500195

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    Where the action is: We synthesized a new series of chloroquine (CQ) analogues characterized by a side chain terminated with a bulky basic head group. Most compounds were found to be active against the D-10 (CQ-susceptible) and W-2 (CQ-resistant) strains of Plasmodium falciparum, with nanomolar and sub-micromolar IC50 values. Four derivatives appear to be of particular interest in terms of their high potency and low cytotoxicity.

  4. N′-Alkylaminosulfonyl Analogues of 6-Fluorobenzylideneindolinones with Desirable Physicochemical Profiles and Potent Growth Inhibitory Activities on Hepatocellular Carcinoma

    Dr. Xiao Chen, Dr. Tianming Yang, Amudha Deivasigamani, Dr. Muthu K. Shanmugam, Prof. Kam-Man Hui, Prof. Gautam Sethi and Prof. Mei-Lin Go

    Article first published online: 21 JUL 2015 | DOI: 10.1002/cmdc.201500235

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    The importance of being drug-like: When inserted into the benzylideneindolinone scaffold, the N′-alkylsulfonylamino group was found to improve aqueous solubility, PAMPA permeability, and growth inhibitory potency toward malignant cells. The most promising compound in this class, 3-12, is apoptogenic and inhibits the phosphorylation of several receptor tyrosine kinases, most prominently FGFR4 and HER3.

  5. Novel Triazolopyrimidine-Derived Cannabinoid Receptor 2 Agonists As Potential Treatment for Inflammatory Kidney Diseases

    Dr. Matthias Nettekoven, Dr. Jean-Michel Adam, Dr. Stefanie Bendels, Dr. Catarina Bissantz, Dr. Jürgen Fingerle, Dr. Uwe Grether, Dr. Sabine Grüner, Dr. Wolfgang Guba, Dr. Atsushi Kimbara, Dr. Giorgio Ottaviani, Bernd Püllmann, Dr. Mark Rogers-Evans, Dr. Stephan Röver, Dr. Benno Rothenhäusler, Sebastien Schmitt, Dr. Franz Schuler, Dr. Tanja Schulz-Gasch and Dr. Christoph Ullmer

    Article first published online: 21 JUL 2015 | DOI: 10.1002/cmdc.201500218

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    Kidney protection: A series of small-molecule CB2 receptor agonists was identified in a high-throughput screen. Lead optimization work gave access to novel triazolopyrimidine derivatives, highly potent on CB2 and selective over CB1. Optimized compound 39 was efficacious in an in vivo model for kidney ischemia–reperfusion and in an in vivo model of renal fibrosis (unilateral ureter obstruction) upon p.o. administration.