title: Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1.
abstract: Potent antagonists of the integrin α(5)β(1), 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.
authors.affiliation: AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims, Cedex 2, France. benedicte.delouvrie@astrazeneca.com
authors.forename: Bénédicte
authors.initials: B
authors.lastname: Delouvrié
authors.forename: Katherine
authors.initials: K
authors.lastname: Al-Kadhimi
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Arnould
authors.forename: Simon T
authors.initials: ST
authors.lastname: Barry
authors.forename: Darren A E
authors.initials: DA
authors.lastname: Cross
authors.forename: Myriam
authors.initials: M
authors.lastname: Didelot
authors.forename: Paul R
authors.initials: PR
authors.lastname: Gavine
authors.forename: Hervé
authors.initials: H
authors.lastname: Germain
authors.forename: Craig S
authors.initials: CS
authors.lastname: Harris
authors.forename: Adina M
authors.initials: AM
authors.lastname: Hughes
authors.forename: David A
authors.initials: DA
authors.lastname: Jude
authors.forename: Jane
authors.initials: J
authors.lastname: Kendrew
authors.forename: Christine
authors.initials: C
authors.lastname: Lambert-van der Brempt
authors.forename: Jean-Jacques
authors.initials: JJ
authors.lastname: Lohmann
authors.forename: Morgan
authors.initials: M
authors.lastname: Ménard
authors.forename: Andrew A
authors.initials: AA
authors.lastname: Mortlock
authors.forename: Martin
authors.initials: M
authors.lastname: Pass
authors.forename: Claire
authors.initials: C
authors.lastname: Rooney
authors.forename: Michel
authors.initials: M
authors.lastname: Vautier
authors.forename: Jennifer L
authors.initials: JL
authors.lastname: Vincent
authors.forename: Nicolas
authors.initials: N
authors.lastname: Warin
mesh_terms: D002448:Cell Adhesion / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D005340:Fibrinogen / Q000737:chemistry; D005353:Fibronectins / Q000737:chemistry; D006801:Humans; D039081:Integrin alpha5beta1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020014:K562 Cells; D008958:Models, Molecular; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D012709:Serum Albumin / Q000737:chemistry; D013329:Structure-Activity Relationship; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D005353:Fibronectins; D039081:Integrin alpha5beta1; D009842:Oligopeptides; D012709:Serum Albumin; D014443:Tyrosine; C047981:arginyl-glycyl-aspartic acid; D005340:Fibrinogen