Thiophene-based vitronectin receptor antagonists

A series of αvβ3 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 αIIbβ3, αvβ5 and α5β1 at the cellular level. In addition, these antagonists exerted an antiangiogenic effect in the chick chorioallantoic membrane (CAM) assay.