Cover image for Vol. 10 Issue 3

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 75/256 (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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February 24, 2015

Editor's Picks: Issue 03/2015

Editor's Picks: Issue 03/2015Editor's picks for issue 03: Full Papers by Inoue and co-workers and Marco-Contelles, Ismaili, et al. illustrate the wide-ranging applicability of natural products in their use as antibacterial agents and to treat Alzheimer's disease. Read more...

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  1. In Vivo Targeting through Click Chemistry

    Dr. Yevgeny Brudno, Rajiv M. Desai, Brian J. Kwee, Prof. Neel S. Joshi, Dr. Michael Aizenberg and Prof. David J. Mooney

    Article first published online: 20 FEB 2015 | DOI: 10.1002/cmdc.201402527

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    Clicks degrees of separation: Selective targeting of small molecules to intramuscular and intradermal sites was achieved by click chemistry. Click-mediated targeting gave a high degree of specificity for the target sites, and this targeting could be repeated over at least one month through nine administrations. Spatial resolution of two different molecules can be achieved by targeting them to two distinct sites in the same animal by use of orthogonal click chemistries, establishing the possibility of combining incompatible therapies in patients.

  2. Selective Inhibitors of Glutathione Transferase P1 with Trioxane Structure as Anticancer Agents

    Maria Bräutigam, Prof. Dr. Nicole Teusch, Tobias Schenk, Miriam Sheikh, Rocky Z. Aricioglu, Swantje H. Borowski, Dr. Jörg-Martin Neudörfl, Prof. Dr. Ulrich Baumann, Prof. Dr. Axel G. Griesbeck and Dr. Markus Pietsch

    Article first published online: 18 FEB 2015 | DOI: 10.1002/cmdc.201402553

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    Peroxides in tumor defense: A dozen cyclic peroxides were prepared by singlet oxygen ene reaction. Investigation of these compounds against tumor-relevant glutathione transferase P1 (GSTP1) revealed Ki values in the low micromolar range. Some inhibitors showed high selectivity for GSTP1 over other GST classes. These findings have strong implications for medicinal chemistry strategies to improve the activity of antitumor drugs.

  3. Looking for Efficient G-Quadruplex Ligands: Evidence for Selective Stabilizing Properties and Telomere Damage by Drug-Like Molecules

    Dr. Bruno Pagano, Dr. Jussara Amato, Nunzia Iaccarino, Dr. Chiara Cingolani, Dr. Pasquale Zizza, Dr. Annamaria Biroccio, Prof. Ettore Novellino and Prof. Antonio Randazzo

    Article first published online: 18 FEB 2015 | DOI: 10.1002/cmdc.201402552

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    A great quad workout: Drug-like compounds that show specific G-quadruplex thermal stabilizing effects and the capacity to induce telomeric damage in cancer cells were identified as promising leads for the development of more potent and selective ligands with anticancer activity.

  4. Design and Synthesis of a MAO-B-Selectively Activated Prodrug Based on MPTP: A Mitochondria-Targeting Chemotherapeutic Agent for Treatment of Human Malignant Gliomas

    Prof. Dr. Martyn A. Sharpe, Dr. Junyan Han, Alexandra M. Baskin and Prof. Dr. David S. Baskin

    Article first published online: 11 FEB 2015 | DOI: 10.1002/cmdc.201402562

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    Specificity is key: We developed a MAO-B-activated prodrug, MP-MUS, for the treatment of brain gliomas. MP-MUS is nontoxic, and can be selectively oxidized by MAO-B, which is overexpressed in glioma cells, to form toxic P+-MUS. P+-MUS translocates inside mitochondria passively and alkylates fragile mitochondrial DNA, leading to specific apoptosis of glioma cells, but not normal cells.

  5. Screening and In Vitro Testing of Antifolate Inhibitors of Human Cytosolic Serine Hydroxymethyltransferase (pages 490–497)

    Dr. Alessandro Paiardini, Dr. Alessio Fiascarelli, Dr. Serena Rinaldo, Dr. Frederick Daidone, Dr. Giorgio Giardina, Dr. David R. Koes, Dr. Alessia Parroni, Dr. Giulia Montini, Dr. Marina Marani, Dr. Alessio Paone, Prof. Lee A. McDermott, Prof. Roberto Contestabile and Prof. Francesca Cutruzzolà

    Article first published online: 10 FEB 2015 | DOI: 10.1002/cmdc.201500028

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    Serine hydroxymethyltransferase (SHMT) has been repeatedly hailed as the missing target for cancer chemotherapy. Here, we identify lometrexol as one of the most potent antifolate inhibitors of human cytosolic SHMT (Kd=2±1 μM) known to date. The results reported represent an initial step toward the development of more potent and effective SHMT inhibitors.