Substituted benzocyloheptenes as potent and selective αv integrin antagonists

A novel series of potent and specific αv integrin antagonists has been obtained by aminoalkyl substitutions on benzocyloheptene acetic acids as a rigid GD bioisostere. The preferred compounds 1–2, 1–3 and 1–8, showed nano- to subnanomolar IC50 values on αvβ3 and αvβ5 integrins, with favorable pharmacokinetics.