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-v-beta-3 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.

“Linear and Cyclic Dehydro-beta-Amino Acids as Conformationally Constrained Scaffolds for the Preparation of Bioactive Compounds”

GENTILUCCI, LUCA;VIOLA, ANGELO;TOLOMELLI, ALESSANDRA
2010

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-v-beta-3 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.
Foldamers: Design, Synthesis and Applications
34
34
G. Cardillo; L. Gentilucci; E.Mosconi; A. Viola; A. Tolomelli
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11585/98982
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