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. 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.

  2. 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.

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

    Alba Mascarin, Ibai E. Valverde and Thomas L. Mindt

    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.

  4. Identification of HDAC6-Selective Inhibitors of Low Cancer Cell Cytotoxicity

    Dr. Irina N. Gaisina, Dr. Werner Tueckmantel, Dr. Andrey Ugolkov, Dr. Sida Shen, Dr. Jessica Hoffen, Dr. Oleksii Dubrovskyi, Dr. Andrew Mazar, Dr. Renee A. Schoon, Dr. Daniel Billadeau and Prof. Dr. Alan P. Kozikowski

    Article first published online: 23 NOV 2015 | DOI: 10.1002/cmdc.201500456

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    High or low selectivity: A new class of HDAC inhibitors bearing an isoxazole ring show high potency and selectivity for HDAC6 over HDAC1–3 and HDAC10, while unexpectedly showing little potency in blocking cell growth. These results suggest that HDAC6 inhibition alone is insufficient for disruption of cell growth, and that some degree of class 1 HDAC inhibition is required. The highly selective HDAC6 inhibitors reported herein that are weakly cytotoxic may find use in cancer immune system reactivation.

  5. Discovery of 3-Hydroxy-3-phenacyloxindole Analogues of Isatin as Potential Monoamine Oxidase Inhibitors

    Rati K. P. Tripathi, Dr. Sairam Krishnamurthy and Dr. Senthil R. Ayyannan

    Article first published online: 23 NOV 2015 | DOI: 10.1002/cmdc.201500443

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    Neural benefit: 3-Hydroxy-3-phenacyloxindole analogues were designed, synthesized, and evaluated as MAO-A/-B inhibitors. Most compounds proved to be potent MAO-A inhibitors. Compound 18 (blue) emerged as a lead MAO-A inhibitor. Docking studies revealed the importance of H-bonding and various hydrophobic interactions for stabilization of inhibitor–MAO-A complexes. These results provide a better understanding of the molecular interactions essential to maintain and improve MAO inhibitory activity and selectivity.