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Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 74/254 (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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September 23, 2014

Diederich to Give Bohlmann Lecture

Diederich to Give Bohlmann LectureCongratulations to François Diederich (ETH Zürich), who will be giving this year's Bohlmann Lecture at the Technische Universität Berlin in November. Diederich is a member of ChemMedChem's International Advisory Board, and recently reported on small-molecule inhibitors of trypanothione reductase.

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  1. Design and Structural Analysis of Aromatic Inhibitors of Type II Dehydroquinase from Mycobacterium tuberculosis

    Dr. Nigel I. Howard, Dr. Marcio V. B. Dias, Dr. Fabienne Peyrot, Dr. Liuhong Chen, Dr. Marco F. Schmidt, Prof. Tom L. Blundell and Prof. Chris Abell

    Article first published online: 18 SEP 2014 | DOI: 10.1002/cmdc.201402298

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    Flattening the ring: A range of synthetically tractable biaryl inhibitors of type II dehydroquinase are described. They were designed with aromatic mimetics of the substrate’s non-aromatic six-membered ring. The compounds were used to investigate hydrogen bond acceptor/donor interaction patterns, aided with protein crystallographic studies.

  2. Structure–Activity Relationship of Tumor-Selective 5-Substituted 2-Amino-3-carboxymethylthiophene Derivatives

    Dr. Joice Thomas, Dr. Alenka Jejcic, Peter Vervaeke, Prof. Romeo Romagnoli, Prof. Sandra Liekens, Prof. Jan Balzarini and Prof. Wim Dehaen

    Article first published online: 18 SEP 2014 | DOI: 10.1002/cmdc.201402274

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    Cytostatic potential & tumor selectivity (TS) of a prototype 2-aminothiophene is retained by replacing the ethyl linker between the thiophene and the substituted aryl by a thioalkyl moiety. A SAR of this class of compounds revealed that the 4-alkylphenyl derivatives are more potent and selective anti-T-lymphoma/leukemia agents than the prototype.

  3. Design, Synthesis, and Biological Evaluation of Shikonin and Alkannin Derivatives as Potential Anticancer Agents via a Prodrug Approach

    Dr. Ru-Bing Wang, Dr. Wen Zhou, Dr. Qing-Qing Meng, Dr. Xu Zhang, Jing Ding, Yan Xu, Hua-Long Song, Dr. Kai Yang, Dr. Jia-Hua Cui and Prof. Shao-Shun Li

    Article first published online: 18 SEP 2014 | DOI: 10.1002/cmdc.201402224

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    The A-B-Cs of a prodrug strategy: Group B compounds show good selectivity and low ROS generation and alkylation in vitro. Acetylation of B results in dimethylated diacetyl derivatives C. Like typical prodrugs, group C compounds exhibit no cytotoxicity in vitro, but show tumor inhibition effects akin to the non-acylated analogues B, without in vivo toxicity. Metabolism by rat liver microsomes suggests that group C compounds are indeed prodrugs of group B.

  4. Discovery of a Highly Selective PLD2 Inhibitor (ML395): A New Probe with Improved Physiochemical Properties and Broad-Spectrum Antiviral Activity against Influenza Strains

    Matthew C. O'Reilly, Thomas H. Oguin III, Dr. Sarah A. Scott, Prof. Paul G. Thomas, Dr. Charles W. Locuson, Ryan D. Morrison, Prof. J. Scott Daniels, Prof. H. Alex Brown and Prof. Craig W. Lindsley

    Article first published online: 10 SEP 2014 | DOI: 10.1002/cmdc.201402333

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    PLD2, viral killer! Focused optimization efforts led to the development of ML395, a potent (IC50=360 nM) and >80-fold selective phospholipase D2 (PLD2) inhibitor with improved physiochemical properties, no cytotoxicity, high CNS penetration and a favorable DMPK profile. The PLD2 inhibitors displayed pan-anti-influenza activity across various influenza strains (H1N1, H3N2, H5N1, H7N9).

  5. Comparative Cytotoxicity of Artemisinin and Cisplatin and Their Interactions with Chlorogenic Acids in MCF7 Breast Cancer Cells

    Dr. John O. Suberu, Dr. Isolda Romero-Canelón, Dr. Neil Sulluvan, Prof. Alexei A. Lapkin and Dr. Guy C. Barker

    Article first published online: 10 SEP 2014 | DOI: 10.1002/cmdc.201402285

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    Ironing out the infusion: Strong antagonistic interactions between artemisinin and chlorogenic acids in MCF7 cells has negative implications for the use of Artemisia tea in chemotherapy. It is possible that the chlorogenic acids present sap artemisinin of its potency by chelating cellular iron.