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...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2000-09, Vol.10 (17), p.1995-1999 |
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Hauptverfasser: | , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(00)00399-1 |