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Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists
Françoise Perron-Sierra1, Dominique Saint Dizier, Marc Bertrand
1Institut de Recherches Servier, 125 chemin de Ronde, 78290 Croissy sur Seine, France.
Bioorganic & Medicinal Chemistry Letters
|October 24, 2002
Abstract:
A novel series of potent and specific alpha(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 alpha(v)beta(3) and alpha(v)beta(5) integrins, with favorable pharmacokinetics.