Abstract
The solid-phase synthesis of cyclic RGD peptides containing either one or two furanoid sugar amino acids (SAAs) is reported. Using a cyclization-cleavage approach five peptides were successfully assembled and consecutively tested on their ability to bind to the integrin receptors α vβ 3 and α IIbβ 3. The cyclic tetrapeptide c[RGD-SAA] ( 1) showed the most promising activity in an inhibition assay with an IC 50 of 1.49 μM for the α vβ 3 receptor and 384 nM for the α IIbβ 3 receptor.
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