Tricyclic pharmacophore-based molecules as novel integrin α v β 3 antagonists. Part IV: Preliminary control of α v β 3 selectivity by meta-oriented substitution
To establish the in vivo efficacy of αvβ3/αIIbβ3 dual antagonists possessing a tricyclic pharmacophore, a corresponding αvβ3-selective antagonist was required as a control. We initially took two synthetic approaches to obtain αvβ3-selective antagonists based on the RGD recognition pattern or on modification of the dihedral angle between the central benzene ring and the adjacent heterocycle, but both proved unsuccessful. However, ...
