ChemMedChem

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Editor-in-Chief: Natalia Ortúzar

Impact Factor: 2.968

ISI Journal Citation Reports © Ranking: 2014: 19/59 (Chemistry Medicinal); 83/254 (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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August 28, 2015

VIP: Acyclic Nucleoside Phosphonates as Plasmodium and Human HG(X)PRT Inhibitors

VIP: Acyclic Nucleoside Phosphonates as Plasmodium and Human HG(X)PRT InhibitorsGiven the development of resistance to current antimalarial medications, new treatments with novel modes of action are urgently needed to combat this infectious disease. Acyclic nucleoside phosphonates have been shown to be potent inhibitors of Plasmodium hypoxanthine-guanine-(xanthine) phosphoribosyltransferase [HG(X)PRT], a key enzyme of the parasitic purine nucleotide salvage pathway. Read more...

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Recently Published Articles

  1. Salicylketoximes That Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells

    Dr. Carlotta Granchi, Dr. Yanrong Qian, Dr. Hyang Yeon Lee, Ilaria Paterni, Carolina Pasero, Jessica Iegre, Kathryn E. Carlson, Prof. Dr. Tiziano Tuccinardi, Prof. Dr. Xiaozhuo Chen, Prof. Dr. John A. Katzenellenbogen, Prof. Dr. Paul J. Hergenrother and Prof. Dr. Filippo Minutolo

    Article first published online: 1 SEP 2015 | DOI: 10.1002/cmdc.201500320

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    Blackout in the city! Enhanced glucose uptake is a consequence of the augmented rate of glycolysis that occurs in neoplastic tissues, which is required to supply a sufficient amount of energy for their rapid growth. New salicylketoxime derivatives are able to “turn the lights off” in cancer cells by blocking their glucose uptake by inhibiting the membrane transporter GLUT1.

  2. MS Binding Assays for D1 and D5 Dopamine Receptors

    Patrick Neiens, Dr. Georg Höfner and Prof. Dr. Klaus Theodor Wanner

    Article first published online: 1 SEP 2015 | DOI: 10.1002/cmdc.201500355

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    Radioligands—no longer needed! We describe binding assays for D1 and D5 dopamine receptors using LC–MS as detection technique for an unlabeled reporter ligand. Based on a highly sensitive and rapid LC–ESI-MS/MS quantification method, saturation and competition experiments could be performed. The results indicate that the established MS Binding Assays are an efficient and reliable alternative to conventional radioligand binding assays.

  3. Synthesis and Evaluation of Novel Acyclic Nucleoside Phosphonates as Inhibitors of Plasmodium falciparum and Human 6-Oxopurine Phosphoribosyltransferases

    Dr. Martin M. Kaiser, Dr. Dana Hocková, Tzu-Hsuan Wang, Dr. Martin Dračínský, Dr. Lenka Poštová-Slavětínská, Eliška Procházková, Dr. Michael D. Edstein, Dr. Marina Chavchich, Dr. Dianne T. Keough, Dr. Luke W. Guddat and Dr. Zlatko Janeba

    Article first published online: 25 AUG 2015 | DOI: 10.1002/cmdc.201500322

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    Combating malaria: An efficient inhibition of plasmodial 6-oxopurine phosphoribosyltransferase, a key enzyme of the parasitic purine nucleotide salvage pathway, is a promising way to combat malaria. Novel acyclic nucleoside phosphonates were designed as potent inhibitors of phosphoribosyltransferases, and the mode of their binding in the enzyme active site was studied in detail.

  4. A Bisbenzamidine Phosphonate as a Janus-faced Inhibitor for Trypsin-like Serine Proteases

    Daniela Häußler, Tamara Scheidt, Dr. Marit Stirnberg, Prof. Dr. Torsten Steinmetzer and Prof. Dr. Michael Gütschow

    Article first published online: 25 AUG 2015 | DOI: 10.1002/cmdc.201500319

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    Two fragments, two modes: We designed a Janus-faced serine protease inhibitor by merging two benzamidine fragments, which impart the molecule with either irreversible or reversible inhibitory activity. Unexpected differences in potency toward trypsin-like proteases were found; the compound exhibits remarkable inhibitory activity against human thrombin. This hybrid approach is a useful way to obtain potent and selective inhibitors.

  5. (−)-Tarchonanthuslactone: Design of New Analogues, Evaluation of their Antiproliferative Activity on Cancer Cell Lines, and Preliminary Mechanistic Studies

    Luiz Fernando Toneto Novaes, Dr. Carolina Martins Avila, Dr. Karin Juliane Pelizzaro-Rocha, Dr. Débora Barbosa Vendramini-Costa, Marina Pereira Dias, Dr. Daniela Barreto Barbosa Trivella, Prof. Dr. João Ernesto de Carvalho, Prof. Dr. Carmen Veríssima Ferreira-Halder and Prof. Dr. Ronaldo Aloise Pilli

    Article first published online: 25 AUG 2015 | DOI: 10.1002/cmdc.201500246

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    Fighting the big C: We describe the synthesis of a new family of analogues based on the scaffold of the natural product (−)-tarchonanthuslactone; these compounds were evaluated in vitro against tumor cell lines. We further conducted an initial investigation into the mechanism of action, including the inhibition of phosphatases and glutathione-S-transferase and the production of reactive oxygen species.

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