Thiophene-based vitronectin receptor antagonists

Abstract A series of α v β 3 antagonists based on a thiophene scaffold were synthesized via two routes and evaluated for in vitro biological activity. We have identified several structurally similar antagonists with different selectivities towards α IIb β 3 , α v β 5 and α 5 β 1 at the cellular level. In addition, these antagonists exerted an antiangiogenic effect in the chick chorioallantoic membrane (CAM) assay.