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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Recently Published Articles

  1. Inhibition of Neuroinflammation by Synthetic Androstene Derivatives Incorporating Amino Acid Methyl Esters on Activated BV-2 Microglia

    Jing Wu, Juanjuan Du, Ruinan Gu, Li Zhang, Prof. Xuechu Zhen, Prof. Yuanchao Li, Prof. Hongli Chen, Prof. Biao Jiang and Prof. Longtai Zheng

    Article first published online: 4 MAR 2015 | DOI: 10.1002/cmdc.201500027

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    Protecting the grey matter! Androstenes incorporating amino acid methyl esters were developed against neuroinflammation. Compound 10 markedly suppressed NO production and iNOS, COX-2, TNF-α and IL-6 expression in lipopolysaccharide-induced microglia. Compound 10 also inhibited phosphorylation of mitogen-activated protein kinases and subsequent activator protein-1 activation. These results suggest 10 as a candidate for development as an anti-neurodegenerative agent.

  2. Pharmacophore-Based Design of Novel Oxadiazoles as Selective Sphingosine-1-phosphate (S1P) Receptor Agonists with in vivo Efficacy

    Dr. Anna Quattropani, Dr. Wolfgang H. B. Sauer, Dr. Stefano Crosignani, Jerome Dorbais, Dr. Patrick Gerber, Jerome Gonzalez, Delphine Marin, Dr. Mathilde Muzerelle, Fanny Beltran, Dr. Anthony Nichols, Dr. Katrin Georgi, Dr. Manfred Schneider, Dr. Pierre-Alain Vitte, Valerie Eligert, Laurence Novo-Perez, Jennifer Hantson, Sebastien Nock, Dr. Susanna Carboni, Dr. Adriano Luis Soares de Souza, Dr. Jean-François Arrighi, Dr. Ursula Boschert and Dr. Agnes Bombrun

    Article first published online: 3 MAR 2015 | DOI: 10.1002/cmdc.201402557

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    Optimizing for MS: We report a pharmacophore driven optimization of novel oxadiazoles as selective sphingosine-1-phosphate (S1P) receptor agonists for the treatment of multiple sclerosis. Compared with the pan-S1P receptor agonist fingolimod, selective S1P1 agonist 45 showed inferior efficacy in an experimental autoimmune encephalomyelitis mouse model, while dual S1P1,5 agonist 49 performed comparably with improved properties.

  3. Scaffold Identification of a New Class of Potent and Selective BCRP Inhibitors

    Federico Marighetti, Dr. Kerstin Steggemann, Maria Karbaum and Prof. Dr. Michael Wiese

    Article first published online: 3 MAR 2015 | DOI: 10.1002/cmdc.201402498

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    Blocking transport: In this study, we set out to better define the scaffold of a new class of compounds we recently reported as breast cancer resistance protein (BCRP) inhibitors. We removed or modified one aromatic ring (ring A) with various substituents that were chosen on the basis of their electronic and lipophilic properties. Intriguingly, this aromatic ring is important, yet not essential, for activity.

  4. Synthesis and In Vitro Antiproliferative Activity of Amido and Amino Analogues of the Marine Alkaloid Isogranulatimide

    Hubert Lavrard, Béatrice Salvetti, Prof. Véronique Mathieu, Dr. Frédéric Rodriguez, Prof. Robert Kiss and Dr. Evelyne Delfourne

    Article first published online: 3 MAR 2015 | DOI: 10.1002/cmdc.201500025

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    Marine inspiration: A new series of amido and amino analogues of the marine alkaloid isogranulatimide were synthesized and evaluated against a panel of six tumor cell lines. Two compounds exhibited single-digit micromolar antiproliferative activity, at least one log of magnitude more potent than the natural product.

  5. 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.