Substituted benzocyloheptenes as potent and selective αv integrin antagonists

Abstract A novel series of potent and specific α v 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 IC 50 values on α v β 3 and α v β 5 integrins, with favorable pharmacokinetics.