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Bioorg Med Chem Lett. 2004 Jun 7;14(11):2905-9.

N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists.

Author information

1
Chemistry Research and Discovery, Amgen Inc., One Amgen Center Dr., Thousand Oaks, CA 91320, USA.

Abstract

Novel alphavbeta3 antagonists based on the N-aryl-gamma-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for alphavbeta3 receptor with excellent selectivity against the structurally related alpha(IIb)beta3 receptor. Additional interactions of N-aryl-gamma-lactam derivatives with alphavbeta3 were found when compared to c(-RGDf[NMe]V-) peptide antagonist. The effects of the conformation and configuration of the gamma-lactam core on the binding were also assessed.

PMID:
15125957
DOI:
10.1016/j.bmcl.2004.03.033
[Indexed for MEDLINE]

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