Homo- and heterodimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part I: Synthesis.
Leonardo Manzoni, Laura Belvisi, Aldo Bianchi, Annalisa Conti, Carmelo Drago, Marilenia de Matteo, Luca Ferrante, Eloise Mastrangelo, Paola Perego, Donatella Potenza, Carlo Scolastico, Federica Servida, Gabriele Timpano, Francesca Vasile, Vincenzo Rizzo, Pierfausto Seneci
Istituto di Scienze e Tecnologie Molecolari (ISTM), Consiglio Nazionale delle Ricerche (CNR), Via Golgi 19, Milan, Italy.
Bioorganic & medicinal chemistry 2012 Nov 15Novel pro-apoptotic, homo- and heterodimeric Smac mimetics/IAPs inhibitors based on the N-AVPI-like 4-substituted 1-aza-2-oxobicyclo[5.3.0]decane scaffold were prepared from monomeric structures connected through a head-head (8), tail-tail (9) or head-tail (10) linker. The selection of appropriate decorating functions for the scaffolds, and of rigid and flexible linkers connecting them, is described. The synthesis, purification and analytical characterization of each prepared dimer 8-10 is thoroughly described. Copyright © 2012 Elsevier Ltd. All rights reserved.
Citation
Leonardo Manzoni, Laura Belvisi, Aldo Bianchi, Annalisa Conti, Carmelo Drago, Marilenia de Matteo, Luca Ferrante, Eloise Mastrangelo, Paola Perego, Donatella Potenza, Carlo Scolastico, Federica Servida, Gabriele Timpano, Francesca Vasile, Vincenzo Rizzo, Pierfausto Seneci. Homo- and heterodimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part I: Synthesis. Bioorganic & medicinal chemistry. 2012 Nov 15;20(22):6687-708
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PMID: 23036335
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