title: Non-peptidic alpha(v)beta3 antagonists containing indol-1-yl propionic acids.
abstract: We describe the synthesis and structure/activity relationship of RGD mimetics that are potent inhibitors of the integrin alpha(v)beta3. Indol-1-yl propionic acids containing a variety of basic moieties at the 5-position, as well as substitutions alpha and beta to the carboxy terminus were synthesized and evaluated. Novel compounds with improved potency have been identified.
authors.affiliation: Johnson & Johnson, Pharmaceutical Research and Development, L.L.C., 665, Stockton Drive, Exton, PA 19341, USA.
authors.forename: Kristi
authors.initials: K
authors.lastname: Leonard
authors.forename: Wenxi
authors.initials: W
authors.lastname: Pan
authors.forename: Beth
authors.initials: B
authors.lastname: Anaclerio
authors.forename: Joan M
authors.initials: JM
authors.lastname: Gushue
authors.forename: Zihong
authors.initials: Z
authors.lastname: Guo
authors.forename: Renee L
authors.initials: RL
authors.lastname: DesJarlais
authors.forename: Marge A
authors.initials: MA
authors.lastname: Chaikin
authors.forename: Jennifer
authors.initials: J
authors.lastname: Lattanze
authors.forename: Carl
authors.initials: C
authors.lastname: Crysler
authors.forename: Carl L
authors.initials: CL
authors.lastname: Manthey
authors.forename: Bruce E
authors.initials: BE
authors.lastname: Tomczuk
authors.forename: Juan Jose
authors.initials: JJ
authors.lastname: Marugan
mesh_terms: D007211:Indoles / Q000737:chemistry; D039302:Integrin alphaVbeta3 / Q000037:antagonists & inhibitors*; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000737:chemistry; D011422:Propionates / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D039302:Integrin alphaVbeta3; D009842:Oligopeptides; D011422:Propionates; C047981:arginyl-glycyl-aspartic acid; C029658:propionic acid