Cover image for Vol. 9 Issue 12

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 75/256 (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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December 18, 2014

The Year in (Mini)Review!

The Year in (Mini)Review!ChemMedChem Volume 9 saw a great number of high-quality secondary publications. The four special issues published in 2014 hosted some particularly insightful Review and Minireview articles written by experts in their fields. All reviews published in ChemMedChem are meant to provide concise yet comprehensive summaries and analysis of recent developments within a given subtopic of medicinal chemistry, which should benefit both seasoned researchers as well as scientists just starting their careers. Read more...

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Recently Published Articles

  1. “Squalenoylcurcumin” Nanoassemblies as Water-Dispersible Drug Candidates with Antileishmanial Activity

    Dr. Zakaria Cheikh-Ali, Dr. Joachim Caron, Dr. Sandrine Cojean, Dr. Christian Bories, Prof. Patrick Couvreur, Prof. Philippe M. Loiseau, Dr. Didier Desmaële, Prof. Erwan Poupon and Prof. Pierre Champy

    Article first published online: 18 DEC 2014 | DOI: 10.1002/cmdc.201402449

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    Curing with curcumin: Two squalenoyl conjugates of the dietary polyphenol curcumin were synthesized by esterification of one or two phenol groups. The polyisoprenoyl appendage allowed self-assembly into nanoparticles 100–150 nm in size that are dispersible in water, show better activity against Leishmania donovani promastigotes than curcumin, and are active against intramacrophagic amastigotes.

  2. Discovery of Mono- and Disubstituted 1H-Pyrazolo[3,4]pyrimidines and 9H-Purines as Catalytic Inhibitors of Human DNA Topoisomerase IIα

    Barbara Pogorelčnik, Dr. Matjaž Brvar, Prof. Bojana Žegura, Prof. Metka Filipič, Prof. Tom Solmajer and Prof. Andrej Perdih

    Article first published online: 17 DEC 2014 | DOI: 10.1002/cmdc.201402459

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    Anticancer target revisited: In a two-stage virtual screening campaign, we discovered novel catalytic inhibitors that target the human DNA topoisomerase IIα ATP binding site. The binding of a new class of pyrazolopyrimidines was fully characterized by surface plasmon resonance experiments. In subsequent optimization, compounds with promising cytotoxicity against HepG2 and MCF-7 cancer cell lines were identified.

  3. Rational Design, Synthesis, and Biological Evaluation of Lactam-Bridged Gramicidin A Analogues: Discovery of a Low-Hemolytic Antibacterial Peptide

    Dr. Ji Mao, Dr. Takefumi Kuranaga, Dr. Hiroshi Hamamoto, Prof. Dr. Kazuhisa Sekimizu and Prof. Dr. Masayuki Inoue

    Article first published online: 15 DEC 2014 | DOI: 10.1002/cmdc.201402473

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    Channel your inner helix: The antibiotic gramicidin A (GA) folds into a β6.3 helix and functions as an ion channel in the cell membrane. We describe the rational design, synthesis, and biological evaluation of lactam-bridged GA analogues. One of them, with a 27-membered macrolactam ring, not only adopts a stable β6.3-helical conformation, but also exhibits high antibacterial activity and significantly decreased hemolytic/cytotoxic activities. This study charts a rational path forward for the development of new ion-channel-based antibiotics.

  4. Investigating the Anti-leishmanial Effects of Linear Peptoids

    Dr. Gabriela A. Eggimann, Hannah L. Bolt, Dr. Paul W. Denny and Dr. Steven L. Cobb

    Article first published online: 15 DEC 2014 | DOI: 10.1002/cmdc.201402416

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    L. mex.­ meets its match: Peptoids—a class of peptide mimetics—have demonstrated their activities against a range of bacterial infections. In this work, we studied the anti-leishmanial properties of linear peptoids, which were observed to have promising activity against Leishmania mexicana axenic amastigotes, a causative agent of cutaneous leishmaniasis.

  5. Electrochemical and mARC-Catalyzed Enzymatic Reduction of para-Substituted Benzamidoximes: Consequences for the Prodrug Concept “Amidoximes instead of Amidines”

    Eva Bauch, Dr. Debora Reichmann, Prof. Dr. Ralf-Rainer Mendel, Dr. Florian Bittner, Anne-Marie Manke, Prof. Dr. Philipp Kurz, Dr. Ulrich Girreser, Dr. Antje Havemeyer and Prof. Dr. Bernd Clement

    Article first published online: 15 DEC 2014 | DOI: 10.1002/cmdc.201402437

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    Fundamental differences between the electrochemical and enzymatic reduction of para-substituted benzamidoximes were detected: The electrochemical properties of the substituent clearly influence the redox potential, but not the enzymatic bioactivation of amidoxime prodrugs.