Synthesis and Biological Investigation of Novel Tricyclic Benzodiazepinedione-Based RGD Analogues

Elisabeth Addicks, Ralph Mazitschek, Athanassios Giannis

ChemBioChem · 2002 · 23 citations · 0 references

Concepts

Abstract

Integrins, a widely expressed family of heterodimeric cell surface adhesion proteins, are expressed in a variety of cell types. They play a decisive role in cell-cell adhesion or cell to extracellular matrix adhesion events. Antagonists of alpha(v)beta(3) or alpha(IIb)beta(3) integrin may have a potential use in suppression of pathological processes. We present the synthesis of novel tricyclic benzodiazepinedione-based RGD analogues, which were subsequently tested in a solid-phase receptor assay in order to investigate their binding affinities towards alpha(v)beta(3) and alpha(IIb)beta(3) integrin.