Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics

In this paper, we describe the synthesis of a selected library of heterochiral d-Pro-containing RGD-peptidomimetics (RpD) and we investigate the biological activity as inhibitors of fibronectin adhesion to SK-MEL-24 tumor cells. In particular, peptides 4 and 8 showed an IC50 in the 10−8 M range. Despite the linear structure, the peptides tend to adopt a folded conformation in a polar environment.