Cover image for Vol. 12 Issue 18

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. Structure-Activity Relationship within a new series at σ₁ and σ₂R ligands: identification of a novel σ₂R agonist (BS148) with selective toxicity against metastatic melanoma

    Livio Brasili, Silvia Franchini, Claudia Sorbi, Umberto M Battisti, Annalisa Tait, Leda I Bancheva, Elena Cichero, Paola Fossa, Antonio Cilia, Orazio Prezzavento, Simone Ronsisvalle, Giuseppina Aricò, Luisa Benassi, Cristina Vaschieri, Paola Azzoni and Cristina Magnoni

    Accepted manuscript online: 22 SEP 2017 04:21AM EST | DOI: 10.1002/cmdc.201700427

  2. Sulfocoumarin-, Coumarin-, 4-Sulfamoylphenyl-Bearing Indazole-3-carboxamide Hybrids: Synthesis and Selective Inhibition of Tumor-Associated Carbonic Anhydrase Isozymes IX and XII

    Srinivas Angapelly, P. V. Sri Ramya, Andrea Angeli, Prof. Claudiu T. Supuran and Dr. Mohammed Arifuddin

    Version of Record online: 22 SEP 2017 | DOI: 10.1002/cmdc.201700446

    Thumbnail image of graphical abstract

    Taking aim at hypoxic tumors: A novel series of sulfocoumarin-, coumarin-, and 4-sulfamoylphenyl-bearing indazole-3-carboxamide hybrids were synthesized and investigated as inhibitors of human carbonic anhydrase (hCA, EC isoforms I, II, IX, and XII. Most of these compounds displayed excellent potency and selectivity against hCA isoforms IX and XII, which have been recently validated as antitumor drug targets.

  3. Opioid Tripeptides Hybridized with trans-1-Cinnamylpiperazine as Proliferation Inhibitors of Pancreatic Cancer Cells in Two- and Three-Dimensional in vitro Models

    Anna K. Laskowska, Anna K. Puszko, Dr. Piotr Sosnowski, Krzysztof Różycki, Dr. Piotr Kosson, Joanna Matalińska, Prof. Marek Durlik and Prof. Aleksandra Misicka

    Version of Record online: 21 SEP 2017 | DOI: 10.1002/cmdc.201700453

    Thumbnail image of graphical abstract

    Multidimensional potency: Pancreatic cancer is a deadly disease resistant to most chemotherapeutics. We synthesized a series of peptidomimetics that are hybrids of opioid tripeptides and trans-1-cinnamylpiperazine. These compounds showed good bioactivity against pancreatic cancer cells in in vitro models. They were especially efficient against spheroids obtained from isolated carcinoma cells. Moreover, these hybrids are stable in plasma up to four days and exhibit very low hemotoxicity.

  4. Synthesis and Evaluation of In Vitro Biological Properties of Ferrocenyl Side-Chain-Decorated Paclitaxel

    Damian Plażuk, Anna Wieczorek, Wojciech M. Ciszewski, Karolina Kowalczyk, Andrzej Błauż, Sylwia Pawlędzio, Anna Makal, Chatchakorn Eurtivong, Homayon J. Arabshahi, Jóhannes Reynisson, Christian G. Hartinger and Błażej Rychlik

    Accepted manuscript online: 21 SEP 2017 02:15AM EST | DOI: 10.1002/cmdc.201700576

  5. Functional N-Formyl Peptide Receptor 2 (FPR2) Antagonists Based on Ureidopropanamide Scaffold Have Potential to Protect Against Inflammation-associated Oxidative Stress.

    Madia Letizia Stama, Enza Lacivita, Liliya N. Kirpotina, Mauro Niso, Roberto Perrone, Igor A. Schepetkin, Mark T. Quinn and Marcello Leopoldo

    Accepted manuscript online: 18 SEP 2017 07:40AM EST | DOI: 10.1002/cmdc.201700429