959991-75-4Relevant academic research and scientific papers
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: Part 2
Delouvrie, Benedicte,Al-Kadhimi, Katherine,Arnould, Jean-Claude,Barry, Simon T.,Cross, Darren A.E.,Didelot, Myriam,Gavine, Paul R.,Germain, Herve,Harris, Craig S.,Hughes, Adina M.,Jude, David A.,Kendrew, Jane,Lambert-Van Der Brempt, Christine,Lohmann, Jean-Jacques,Menard, Morgan,Mortlock, Andrew A.,Pass, Martin,Rooney, Claire,Vautier, Michel,Vincent, Jennifer L.,Warin, Nicolas
scheme or table, p. 4117 - 4121 (2012/07/03)
Potent antagonists of the integrin α5β1, 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.
N-(BENZOYL)-O- [2- (PYRIDIN- 2 -YLAMINO) ETHYL] -L-TYROSINE DERIVATIVES AND RELATED COMPOUNDS AS A5B1 ANTAGONISTS FOR THE TREATMENT OF SOLID TUMORS
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Page/Page column 219; 220, (2008/06/13)
The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to a5b1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins.
