Nonpeptide RGD antagonists: A novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam

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Abstract

The 1-azabicyclo[5.2.0]nonan-2-one lactam 1 adequately substituted on both cycles A and B as scaffolds mimics the conformationally constrained β-turn of the tripeptide RGD signaling motif of fibronectin. Using an in vitro assay, we establish that trans diastereoisomer 1b dissociates a soluble fibronectin-integrin α5β1 complex at concentrations comparable to those of a linear RGDS peptide as a competitor. © 2003 Elsevier Science Ltd. All rights reserved.

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Bourguet, E., Banères, J. L., Parello, J., Lusinchi, X., Girard, J. P., & Vidal, J. P. (2003). Nonpeptide RGD antagonists: A novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam. Bioorganic and Medicinal Chemistry Letters, 13(9), 1561–1564. https://doi.org/10.1016/S0960-894X(03)00181-1

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