Structure–activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: Part 1

Potent antagonists of the integrin α5β1, which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-06, Vol.22 (12), p.4111-4116
Hauptverfasser:	Delouvrié, Bénédicte, Al-Kadhimi, Katherine, Arnould, Jean-Claude, Barry, Simon T., Cross, Darren A.E., Didelot, Myriam, Gavine, Paul R., Germain, Hervé, Harris, Craig S., Hughes, Adina M., Jude, David A., Kendrew, Jane, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Ménard, Morgan, Mortlock, Andrew A., Pass, Martin, Rooney, Claire, Vautier, Michel, Vincent, Jennifer L., Warin, Nicolas
Format:	Artikel
Sprache:	eng
Schlagworte:	Angiogenesis antagonists Biological and medical sciences Cell Adhesion - drug effects Cell Survival - drug effects Fibrinogen - chemistry Fibronectins - chemistry Humans Integrin alpha5beta1 - antagonists & inhibitors Integrin alpha5beta1 - metabolism Integrin α5β1 antagonist integrins K562 Cells Medical sciences Models, Molecular Molecular Mimicry Oligopeptides - chemical synthesis Oligopeptides - pharmacology Pharmacology. Drug treatments RGD integrin Serum Albumin - chemistry Structure-Activity Relationship structure-activity relationships tyrosine Tyrosine - analogs & derivatives Tyrosine - chemical synthesis Tyrosine - pharmacology Zwitterion
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Beschreibung
Zusammenfassung:	Potent antagonists of the integrin α5β1, which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.04.063