Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids

N,N-Dicinnamyl, N-benzyl- N-cinnamyl, and N,N-dibenzyl amino acids were prepared and evaluated in an EPO binding assay. Several derivatives of aspartic acid, glutamic acid, and lysine exhibited moderate (10–50 μM) affinity for EBP; ‘dimerization’ of the most potent analogues by coupling with linear...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry letters 2000-09, Vol.10 (17), p.1995-1999
Hauptverfasser: Connolly, Peter J, Wetter, Steven K, Murray, William V, Johnson, Dana L, McMahon, Frank J, Farrell, Francis X, Tullai, Jennifer, Jolliffe, Linda K
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:N,N-Dicinnamyl, N-benzyl- N-cinnamyl, and N,N-dibenzyl amino acids were prepared and evaluated in an EPO binding assay. Several derivatives of aspartic acid, glutamic acid, and lysine exhibited moderate (10–50 μM) affinity for EBP; ‘dimerization’ of the most potent analogues by coupling with linear diamines led to EPO competitors having 1–2 μM binding affinities.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00399-1