• Title of article

    Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy Original Research Article

  • Author/Authors

    Pierfausto Seneci، نويسنده , , Aldo Bianchi، نويسنده , , Cristina Battaglia، نويسنده , , Laura Belvisi، نويسنده , , Martino Bolognesi، نويسنده , , Andrea Caprini، نويسنده , , Federica Cossu، نويسنده , , Elena de Franco، نويسنده , , Marilenia de Matteo، نويسنده , , Domenico Delia، نويسنده , , Carmelo Drago، نويسنده , , Amira Khaled، نويسنده , , Daniele Lecis، نويسنده , , Leonardo Manzoni، نويسنده , , Moira Marizzoni، نويسنده , , Elo، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2009
  • Pages
    23
  • From page
    5834
  • To page
    5856
  • Abstract
    Novel proapoptotic Smac mimics/IAPs inhibitors have been designed, synthesized and characterized. Computational models and structural studies (crystallography, NMR) have elucidated the SAR of this class of inhibitors, and have permitted further optimization of their properties. In vitro characterization (XIAP BIR3 and linker-BIR2–BIR3 binding, cytotox assays, early ADMET profiling) of the compounds has been performed, identifying one lead for further in vitro and in vivo evaluation.
  • Keywords
    Smac , XIAP , apoptosis , Oncology , rational drug design , NMR , medicinal chemistry , Crystallography
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Serial Year
    2009
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Record number

    1306251

    • Link To Document
    https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=1306251