title: RGD mimetics containing a central hydantoin scaffold: alpkha(v)beta3 vs alpha(IIb)beta3 selectivity requirements.
abstract: The synthesis of a series of RGD mimetic alpha(v)beta3 antagonists containing a hydantoin scaffold is shown. The results demonstrate some of the structural requirements for the design of selective alpha(v)beta3 antagonists (vs alpha(IIb)beta3) in terms of the Arg-mimetic, the distance between N- and C-terminus and the lipophilic side chain.
authors.affiliation: Hoechst Marion Roussel Deutschland GmhH, Frankfurt, Germany. anusch.peyman@hmrag.com
authors.forename: A
authors.initials: A
authors.lastname: Peyman
authors.forename: V
authors.initials: V
authors.lastname: Wehner
authors.forename: J
authors.initials: J
authors.lastname: Knolle
authors.forename: H U
authors.initials: HU
authors.lastname: Stilz
authors.forename: G
authors.initials: G
authors.lastname: Breipohl
authors.forename: K H
authors.initials: KH
authors.lastname: Scheunemann
authors.forename: D
authors.initials: D
authors.lastname: Carniato
authors.forename: J M
authors.initials: JM
authors.lastname: Ruxer
authors.forename: J F
authors.initials: JF
authors.lastname: Gourvest
authors.forename: T R
authors.initials: TR
authors.lastname: Gadek
authors.forename: S
authors.initials: S
authors.lastname: Bodary
mesh_terms: D005340:Fibrinogen / Q000378:metabolism; D006801:Humans; D006827:Hydantoins / Q000138:chemical synthesis*; D007093:Imidazoles / Q000138:chemical synthesis; D015394:Molecular Structure; D009842:Oligopeptides / Q000138:chemical synthesis*; D010455:Peptides / Q000378:metabolism; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000378:metabolism; D011485:Protein Binding / Q000187:drug effects; D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors
chemical_list: D006827:Hydantoins; D007093:Imidazoles; D009842:Oligopeptides; D010455:Peptides; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D019030:Receptors, Vitronectin; C047981:arginyl-glycyl-aspartic acid; C067623:kistrin; D005340:Fibrinogen