Cover image for Vol. 12 Issue 15

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. Trifluoromethyl Oxetanes: Synthesis and Evaluation as a tert-Butyl Isostere

    Paramita Mukherjee, Martin Pettersson, Jason K. Dutra, Longfei Xie and Christopher W. am Ende

    Accepted manuscript online: 16 AUG 2017 10:20AM EST | DOI: 10.1002/cmdc.201700333

  2. Biophysical Screening of a Focused Library for the Discovery of CYP121 Inhibitors as Novel Antimycobacterials

    Christian Brengel, Andreas Thomann, Alexander Schifrin, Giuseppe Allegretta, Ahmed A. M. Kamal, Joerg Haupenthal, Isabell Schnorr, Sang Hyun Cho, Scott Gary Franzblau, Martin Empting, Jens Eberhard and Rolf W Hartmann

    Accepted manuscript online: 16 AUG 2017 03:20AM EST | DOI: 10.1002/cmdc.201700363

  3. Design and synthesis of terephthalic acid-based histone deacetylase inhibitors with dual stage anti-Plasmodium activity

    Katharina Stenzel, Ming Jang Chua, Sandra Duffy, Yevgeniya Antonova-Koch, Stephan Meister, Alexandra Hamacher, Matthias U. Kassack, Elizabeth A. Winzeler, Vicky M. Avery, Thomas Kurz, Katherine T. Andrews and Finn Kristian Hansen

    Accepted manuscript online: 15 AUG 2017 09:21PM EST | DOI: 10.1002/cmdc.201700360

  4. Direct and Topoisomerase II Mediated DNA Damage by Bis-3-chloropiperidines: The Importance of Being an Earnest G

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

    Version of Record online: 10 AUG 2017 | DOI: 10.1002/cmdc.201700368

    Thumbnail image of graphical abstract

    The assault on guanines! In exploring the molecular details of the reactivity of bis-3-chloropiperidines with DNA, our results demonstrate that the initial attack is directed toward the N7 position of guanine, generating both mono- and bi-functional adducts. The DNA damage inflicted by bis-3-chloropiperidines has meaningful properties on the activity of human topoisomerases IIα to develop this class of DNA-active compounds as anticancer agents.

  5. Heme Oxygenase Database (HemeOxDB) and QSAR Analysis of Isoform 1 Inhibitors

    Dr. Emanuele Amata, Prof. Agostino Marrazzo, Dr. Maria Dichiara, Dr. Maria N. Modica, Prof. Loredana Salerno, Prof. Orazio Prezzavento, Dr. Giovanni Nastasi, Prof. Antonio Rescifina, Prof. Giuseppe Romeo and Dr. Valeria Pittalà

    Version of Record online: 9 AUG 2017 | DOI: 10.1002/cmdc.201700321

    Thumbnail image of graphical abstract

    Heme oxygenase inhibitors: A collection of the whole set of heme oxygenase (HO) inhibitors is reported, and inhibitors of heme oxygenase-1 (HO-1) were used in creating a Monte Carlo based QSAR model. The screening of a number of FDA-approved drugs with the developed model revealed that top-scored compounds share common sulfonylurea or sulfonyl acetamide functions, which may be novel replacements for the imidazole used in the vast majority of HO-1 inhibitors.