Cover image for Vol. 10 Issue 12

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 2.968

ISI Journal Citation Reports © Ranking: 2014: 19/59 (Chemistry Medicinal); 83/255 (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 24, 2015

Editor's Picks: Issue 12/2015

Editor's Picks: Issue 12/2015The Editor's picks for issue 12 report studies that address aberrant lipid metabolism. The Full Paper by Overkleeft, Aerts, and colleagues is focused on three enzymes involved in the metabolism of glucosylceramide, while another Full Paper by Tacke and co-workers discusses silicon-containing agonists of receptors that mediate antilipolytic effects. Read more...

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  1. Design, Synthesis and Evaluation of Triazole-Pyrimidine Analogues as SecA Inhibitors

    Jianmei Cui, Jinshan Jin, Arpana Sagwal Chaudhary, Ying-hsin Hsieh, Hao Zhang, Chaofeng Dai, Krishna Damera, Weixuan Chen, Phang C. Tai and Binghe Wang

    Article first published online: 26 NOV 2015 | DOI: 10.1002/cmdc.201500447

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    One stone, several birds! The SecA inhibitors discovered in this study are broad-spectrum antimicrobials with the intrinsic ability to null the effect of efflux pumps. They are therefore effective against multidrug-resistant bacterial strains, can inhibit virulence factor secretion, and are very active against strains of bacteria that are resistant to antibiotics in current use, including vancomycin.

  2. Inspired by Nature: The 3-Halo-4,5-dihydroisoxazole Moiety as a Novel Molecular Warhead for the Design of Covalent Inhibitors

    Dr. Andrea Pinto, Dr. Lucia Tamborini, Dr. Gregorio Cullia, Prof. Paola Conti and Prof. Carlo De Micheli

    Article first published online: 26 NOV 2015 | DOI: 10.1002/cmdc.201500496

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    A hint from Nature: 3-Halo-4,5-dihydroisoxazole, a component of the naturally occurring antibiotic acivicin, is a powerful warhead for the covalent inhibition of target enzymes. Here, we describe the use of this moiety in medicinal chemistry to develop covalent inhibitors of parasitic and bacterial enzymes, and human targets involved in the modulation of neuronal metabolic pathways or tumor cell metabolism.

  3. Designing Irreversible Inhibitors—Worth the Effort?

    Prof. Concepción González-Bello

    Article first published online: 23 NOV 2015 | DOI: 10.1002/cmdc.201500469

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    No backing out: For many years, medicinal chemists have generally steered clear of irreversible inhibitors, given the relatively high risk they pose in terms of off-target effects. However, the unique benefits of irreversible inhibition are gathering more attention, as further knowledge is gained about the challenging mechanisms behind covalent modification for certain compound classes.

  4. Photoinduced Isomerization and Hepatoxicities of Semaxanib, Sunitinib and Related 3-Substituted Indolin-2-ones

    Dr. Mun Hong Ngai, Choon Leng So, Dr. Michael B. Sullivan, Prof. Dr. Han Kiat Ho and Prof. Dr. Christina L. L. Chai

    Article first published online: 23 NOV 2015 | DOI: 10.1002/cmdc.201500475

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    Light, isomerization, toxicity: The kinetics of photoisomerization and cytotoxicity of a series of semaxanib analogues were studied. No direct correlation between the rate of photoisomerization and the nature of the C5 substituent was observed. Theoretical calculations predicted that high oscillator strength would lead to photoisomerization. Compounds with a pyrrolic N-methyl substituent were found to be less toxic.

  5. Structure–Activity Relationship Studies of Amino Acid Substitutions in Radiolabeled Neurotensin Conjugates

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    Article first published online: 23 NOV 2015 | DOI: 10.1002/cmdc.201500468

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    A level playing field: Standardized experimental conditions for the preclinical in vitro evaluation of radiolabeled neurotensin [NT(8–13)] derivatives enabled a thorough structure–activity relationship study of the effects of commonly applied amino acid substitutions on the biological properties of these tumor-targeting peptide conjugates.