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. A Hollow NaGdF4/AFn Nanosystem Based on “Relay Race” Release for Therapy

    Dr. Jie Zhou, Dr. Hanchun Yao, Lingchang Meng, Chong Sun, Weiran Ye and Qiuzheng Du

    Version of Record online: 25 JUL 2017 | DOI: 10.1002/cmdc.201700295

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    Pass the baton! We synthesized hollow mesoporous structured NaGdF4 nanoparticles with both excellent upconversion luminescent and magnetic resonance capacities for in vivo imaging applications. The dual-drug system CUR/NaGdF4–DOX/AFn–FA enabled the temporal release of two drugs: curcumin (CUR) is released rapidly to inhibit P-glycoprotein (P-gp) activity and to restore apoptosis signaling pathways, while doxorubicin (DOX) undergoes sustained release and thus high accumulation in drug-resistant cells to exert its therapeutic effect thanks to CUR-mediated inactivation of P-gp.

  2. Discovery of wtRET and V804MRET Inhibitors: From Hit to Lead

    Dr. Luca Mologni, Dr. Martina Dalla Via, Prof. Adriana Chilin, Prof. Manlio Palumbo and Dr. Giovanni Marzaro

    Version of Record online: 25 JUL 2017 | DOI: 10.1002/cmdc.201700243

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    Intentional inhibition: RET kinases are involved in the onset and development of various types of cancer. Currently approved RET inhibitors were not originally designed to be RET inhibitors, and their potency against RET kinase has not been optimized. Starting from our previously identified dual cKIT/PDGFRβ inhibitor, we report the development of a novel multi-cKIT/wtRET/V804MRET inhibitor.

  3. Critical Evaluation of Native Electrospray Ionization Mass Spectrometry for Fragment-Based Screening

    Melanie Göth, Dr. Volker Badock, Dr. Jörg Weiske, Prof. Dr. Kevin Pagel and Dr. Benno Kuropka

    Version of Record online: 25 JUL 2017 | DOI: 10.1002/cmdc.201700177

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    Does mass matter? Defined sets of fragments were screened against four target proteins by using native mass spectrometry (MS). Beside specific complex formation, many fragments show multiple binding and charge-state shifts. These factors complicate automated data analysis and diminish the attractiveness of native MS as a primary fragment screening tool. However, a comparison of the hits identified by native MS and thermal shift assays shows good agreement for two of the target proteins.

  4. Development of a New Structural Class of Broadly Acting HCV Non-Nucleoside Inhibitors Leading to the Discovery of MK-8876

    Dr. Casey C. McComas, Dr. Anandan Palani, Dr. Wei Chang, Dr. M. Katharine Holloway, Dr. Charles A. Lesburg, Dr. Peng Li, Dr. Nigel Liverton, Dr. Peter T. Meinke, Dr. David B. Olsen, Dr. Xuanjia Peng, Dr. Richard M. Soll, Dr. Ajay Ummat, Dr. Jie Wu, Dr. Jin Wu, Dr. Nicolas Zorn and Dr. Steven W. Ludmerer

    Version of Record online: 25 JUL 2017 | DOI: 10.1002/cmdc.201700228

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    Both palms open: Studies directed at developing a broadly acting non-nucleoside inhibitor of HCV NS5B led to the discovery of a novel structural class of 5-aryl benzofurans that simultaneously interact with both the palm I and palm II binding regions. Herein we describe the efforts that led to the discovery of MK-8876, which advanced into Phase 1 monotherapy studies for evaluation and characterization as a component of an all-oral direct-acting drug regimen for the treatment of chronic HCV infection.

  5. Discovery of Novel Potent Muscarinic M3 Receptor Antagonists with Proper Plasma Stability by Structural Recombination of Marketed M3 Antagonists

    Zuojuan Xiang, Prof. Jun Liu, Prof. Hongbin Sun and Prof. Xiaoan Wen

    Version of Record online: 25 JUL 2017 | DOI: 10.1002/cmdc.201700189

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    Steady as she goes: Structural recombination of the marketed muscarinic M3 receptor antagonists aclidinium bromide and glycopyrronium bromide, which have inappropriate plasma stability, led to the discovery of novel potent M3 receptor antagonists 1 a and 1 b, which have proper plasma stability. These antagonists hold great promise as clinical drug candidates to overcome the drawbacks caused by the unsuitable stability of currently marketed M3 antagonists.