Cover image for Vol. 12 Issue 14

Editorial Board Chairs: Karl-Heinz Altmann, Antonello Mai, Rainer Metternich. Editor: David Peralta

Impact Factor: 3.225

ISI Journal Citation Reports © Ranking: 2016: 17/60 (Chemistry Medicinal); 73/256 (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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November 23, 2016

13th WCMBC in Steamboat Springs: January 2017

13th WCMBC in Steamboat Springs: January 2017ChemMedChem will be sponsoring the next Winter Conference on Medicinal & Bioorganic Chemistry this coming January 22nd–26th in Steamboat Springs, Colorado. The organizers have lined up another impressive list of presenters for this year's event. And as if excellent cutting-edge science weren't enough, this meeting comes with a healthy dose of play time too: unforgettable skiing in the bright sun and deep snow of northern Colorado. Make sure to register soon!

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Recently Published Articles

  1. Design and Synthesis of New 4-Alkylidene-beta-lactams: Benzyl-and Phenethyl-carbamate as Key Fragments to Switch on the Antibacterial Activity

    Daria Giacomini, Giulia Martelli, Miriam Piccichè, Enrico Calaresu, Clementina Elvezia Anna Cocuzza and Rosario Musumeci

    Accepted manuscript online: 23 JUL 2017 09:31PM EST | DOI: 10.1002/cmdc.201700307

  2. Direct and Topoisomerase II mediated DNA damage by Bis-3-chloropiperidines: the importance of being an earnest G

    Alice Sosic, Ivonne Zuravka, Nina-Katharina Schmitt, Angelica Miola, Richard Göttlich, Dan Fabris and Barbara Gatto

    Accepted manuscript online: 19 JUL 2017 12:10PM EST | DOI: 10.1002/cmdc.201700368

  3. Rational Design of a Highly Potent and Selective Peptide Inhibitor of PACE4 by Salt Bridge Interaction with D160 at Position P3

    Vahid Dianati, Azar Shamloo, Dr. Anna Kwiatkowska, Roxane Desjardins, Prof. Dr. Armand Soldera, Prof. Dr. Robert Day and Prof. Dr. Yves L. Dory

    Version of Record online: 19 JUL 2017 | DOI: 10.1002/cmdc.201700300

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    Setting the PACE with concurrent control of conformation and binding: Most substrates of proteases form a β-sheet with the active site upon binding. New β-branched residues, known to favor β-sheet conformation in linear peptides, were introduced at the P3 Val position of inhibitors of the serine protease PACE4. Through this P3 strategic position, it was possible to obtain potent and selective inhibitors, by additive β-sheet conformation control and salt bridge formation with PACE4 Asp160.

  4. Effects of Pimozide Derivatives on pSTAT5 in K562 Cells

    Dr. Riccardo Rondanin, Prof. Daniele Simoni, Dr. Martina Maccesi, Prof. Romeo Romagnoli, Prof. Stefania Grimaudo, Dr. Rosaria Maria Pipitone, Dr. Maria Meli, Prof. Antonio Cascio and Dr. Manlio Tolomeo

    Version of Record online: 19 JUL 2017 | DOI: 10.1002/cmdc.201700234

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    Neuroleptic goes anticancer: New derivatives of pimozide were obtained with potent growth inhibitory and apoptotic activity in K562 BCR-ABL-expressing leukemia cell lines. The detection of overexpressed phosphorylated STAT5 with a fluorophore-conjugated monoclonal antibody (anti-pSTAT5) resulted in strong inhibition with derivatives at a concentration of 10–15 μm, in contrast to pimozide, active at 30 μm under the same conditions.

  5. Recent Research Advances in Selective Matrix Metalloproteinase-13 Inhibitors as Anti-Osteoarthritis Agents

    Xin-Wen Xie, Prof. Ren-Zhong Wan and Prof. Zhao-Peng Liu

    Version of Record online: 19 JUL 2017 | DOI: 10.1002/cmdc.201700349

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    Lucky 13: Matrix metalloproteinase-13 (MMP-13) plays a key role in the degradation of type II collagen in cartilage and bone in osteoarthritis (OA). This review covers recent advances in the area of MMP-13-specific inhibitors, which lack the risks associated with the inhibition of other MMP isoforms. With greater insight into the mechanism of action of MMP-13 and the pathogenic process of OA, research into selective MMP-13 inhibitors will make significant breakthroughs for patients suffering from OA in the near future.