Cover image for Vol. 9 Issue 9

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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August 28, 2014

C. A. Olsen interview at ChemistryViews

C. A. Olsen interview at ChemistryViewsChemMedChem author and this year's recipient of the EFMC Prize for a Young Medicinal Chemist in Academia, Professor Christian A. Olsen (University of Copenhagen), recently answered some questions we had about the work behind his paper Effect of Various Zinc Binding Groups on Inhibition of Histone Deacetylases 1–11, which appeared earlier this year in our Special Issue on Epigenetics and Drug Discovery. He also discussed his research projects and goals in general, and what makes his successful research group tick. The full interview can be found at ChemistryViews. Be sure to catch Olsen's Concept article, also in the Epigenetics special issue.

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Recently Published Articles

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    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

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    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.

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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).

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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.