Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 2

  • Bioorg Med Chem Lett. 2012 Jun 15;22(12):4117-21. doi: 10.1016/j.bmcl.2012.04.061.
Bénédicte Delouvrié  1 ,  Katherine Al-Kadhimi ,  Jean-Claude Arnould ,  Simon T Barry ,  Darren A E Cross ,  Myriam Didelot ,  Paul R Gavine ,  Hervé Germain ,  Craig S Harris ,  Adina M Hughes ,  David A Jude ,  Jane Kendrew ,  Christine Lambert-van der Brempt ,  Jean-Jacques Lohmann ,  Morgan Ménard ,  Andrew A Mortlock ,  Martin Pass ,  Claire Rooney ,  Michel Vautier ,  Jennifer L Vincent ,  Nicolas Warin
Affiliations
  • 1. AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims, Cedex 2, France. [email protected]
PMID: 22572578 DOI: 10.1016/j.bmcl.2012.04.061
Abstract

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.