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EnglishIn a project dealing with the stereoselective synthesis of dehydro-beta-amino acids, we envisaged the insertion of these unusual amino acids as rigid cores in small constrained molecules mimicking the RGD motif, a peptidic sequence recognized by different integrin subtypes as alpha--beta3 and alpha-5-beta-1. Three different libraries of derivatives have been synthesized in few steps starting from alkylidene acetoacetates. The biological evaluation of the prepared inhibitors confirmed that these unusual beta-amino acids may represent interesting scaffolds for the preparation of novel anticancer agents.
| Titolo: | Stereoselective Synthesis of Linear and Cyclic Dehydro-beta-amino Acids for the Preparation of alpha-v-beta-3 and alpha-5-beta-1 Integrin Inhibitors |
| Autore/i: | CARDILLO, GIULIANA; GENTILUCCI, LUCA; MOSCONI, ELISA; VIOLA, ANGELO; TOLOMELLI, ALESSANDRA |
| Autore/i Unibo: | |
| Anno: | 2010 |
| Rivista: | |
| Pagina iniziale: | 63 |
| Pagina finale: | 63 |
| Abstract: | In a project dealing with the stereoselective synthesis of dehydro-beta-amino acids, we envisaged the insertion of these unusual amino acids as rigid cores in small constrained molecules mimicking the RGD motif, a peptidic sequence recognized by different integrin subtypes as alpha--beta3 and alpha-5-beta-1. Three different libraries of derivatives have been synthesized in few steps starting from alkylidene acetoacetates. The biological evaluation of the prepared inhibitors confirmed that these unusual beta-amino acids may represent interesting scaffolds for the preparation of novel anticancer agents. |
| Data prodotto definitivo in UGOV: | 23-feb-2011 |
| Appare nelle tipologie: | 4.02 Riassunto (Abstract) |
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