title: Synthesis of highly potent and selective hetaryl ureas as integrin alpha(V)beta3-receptor antagonists.
abstract: Solid-phase synthesis and SAR of integrin alpha(V)beta3-receptor antagonists containing a urea moiety as non-basic guanidine mimetic are described. The most potent compounds exhibited IC(50) values towards alpha(V)beta3 in the nanomolar range and high selectivity versus related integrins like alpha(IIb)beta3. For selected examples efficacy in functional cellular assays is demonstrated.
authors: BASF AG, D-67056, Ludwigshafen, Germany. udo.lange@basf-ag.de
authors: Udo E W
authors: UE
authors: Lange
authors: Gisela
authors: G
authors: Backfisch
authors: Jürgen
authors: J
authors: Delzer
authors: Hervé
authors: H
authors: Geneste
authors: Claudia
authors: C
authors: Graef
authors: Wilfried
authors: W
authors: Hornberger
authors: Andreas
authors: A
authors: Kling
authors: Arnulf
authors: A
authors: Lauterbach
authors: Thomas
authors: T
authors: Subkowski
authors: Christian
authors: C
authors: Zechel
mesh_terms: D000818:Animals; D016466:CHO Cells; D002448:Cell Adhesion / Q000187:drug effects*; D006224:Cricetinae; D015195:Drug Design; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D019030:Receptors, Vitronectin; D014508:Urea