| Literature DB >> 19620011 |
Pierfausto Seneci1, Aldo Bianchi, Cristina Battaglia, Laura Belvisi, Martino Bolognesi, Andrea Caprini, Federica Cossu, Elena de Franco, Marilenia de Matteo, Domenico Delia, Carmelo Drago, Amira Khaled, Daniele Lecis, Leonardo Manzoni, Moira Marizzoni, Eloise Mastrangelo, Mario Milani, Ilaria Motto, Elisabetta Moroni, Donatella Potenza, Vincenzo Rizzo, Federica Servida, Elisa Turlizzi, Maurizio Varrone, Francesca Vasile, Carlo Scolastico.
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.Entities:
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Year: 2009 PMID： 19620011 DOI： 10.1016/j.bmc.2009.07.009
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641