Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 2.
| Autor: | Delouvrié B; AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims, Cedex 2, France. benedicte.delouvrie@astrazeneca.com, Al-Kadhimi K, Arnould JC, Barry ST, Cross DA, Didelot M, Gavine PR, Germain H, Harris CS, Hughes AM, Jude DA, Kendrew J, Lambert-van der Brempt C, Lohmann JJ, Ménard M, Mortlock AA, Pass M, Rooney C, Vautier M, Vincent JL, Warin N |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Jun 15; Vol. 22 (12), pp. 4117-21. Date of Electronic Publication: 2012 Apr 21. |
| DOI: | 10.1016/j.bmcl.2012.04.061 |
| Abstrakt: | Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This paper describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the central aromatic core and the amide moiety. (Copyright © 2012 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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