Synthesis and biological investigation of novel tricyclic benzodiazepinedione-based RGD analogues.
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.
Addicks
Elisabeth
E
Institut für Organische Chemie Universität Leipzig, Johannisallee 29 04103 Leipzig, Germany.
Mazitschek
Ralph
R
Giannis
Athanassios
A
D001570:Benzodiazepinones / Q000138:chemical synthesis*; D001667:Binding, Competitive; D005340:Fibrinogen / Q000037:antagonists & inhibitors; D006575:Heterocyclic Compounds, 3-Ring / Q000138:chemical synthesis*; D016023:Integrins / Q000378:metabolism; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry
D001570:Benzodiazepinones; D006575:Heterocyclic Compounds, 3-Ring; D016023:Integrins; D009842:Oligopeptides; C047981:arginyl-glycyl-aspartic acid; D005340:Fibrinogen