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

Authors
Connolly, PJ Wetter, SK Murray, WV Johnson, DL McMahon, FJ Farrell, FX Tullai, J Jolliffe, LK
Citation
Pj. Connolly et al., Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids, BIOORG MED, 10(17), 2000, pp. 1995-1999
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
17
Year of publication
2000
Pages
1995 - 1999
Database
ISI
SICI code
0960-894X(20000904)10:17<1995:SAERBA>2.0.ZU;2-I
Abstract
N, N-Dicinnamyl, N-benzyl-N-cinnamyl, and N, N-dibenzyl amino acids were pr epared and evaluated in an EPO binding assay. Several derivatives of aspart ic acid, glutamic acid, and lysine exhibited moderate (10 50 mu M) affinity for EBP; 'dimerization' of the most potent analogues by coupling with line ar diamines led to EPO competitors having 1-2 mu M binding. affinities. (C) 2000 Elsevier Science Ltd. All rights reserved.