Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy - PubMed (original) (raw)

. 2009 Aug 15;17(16):5834-56.

doi: 10.1016/j.bmc.2009.07.009. Epub 2009 Jul 10.

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

Affiliations

• PMID: 19620011
• DOI: 10.1016/j.bmc.2009.07.009

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

Pierfausto Seneci et al. Bioorg Med Chem. 2009.

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.

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