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  • Title: Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists.
    Author: Perron-Sierra F, Saint Dizier D, Bertrand M, Genton A, Tucker GC, Casara P.
    Journal: Bioorg Med Chem Lett; 2002 Nov 18; 12(22):3291-6. PubMed ID: 12392735.
    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.
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