title: Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
abstract: A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.
authors.affiliation: Cancer Research, Global Pharmaceutical R&D, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6101, USA. milan.bruncko@abbott.com
authors.forename: Milan
authors.initials: M
authors.lastname: Bruncko
authors.forename: William J
authors.initials: WJ
authors.lastname: McClellan
authors.forename: Michael D
authors.initials: MD
authors.lastname: Wendt
authors.forename: Daryl R
authors.initials: DR
authors.lastname: Sauer
authors.forename: Andrew
authors.initials: A
authors.lastname: Geyer
authors.forename: Christopher R
authors.initials: CR
authors.lastname: Dalton
authors.forename: Michele A
authors.initials: MA
authors.lastname: Kaminski
authors.forename: Moshe
authors.initials: M
authors.lastname: Weitzberg
authors.forename: Jane
authors.initials: J
authors.lastname: Gong
authors.forename: Joseph F
authors.initials: JF
authors.lastname: Dellaria
authors.forename: Robert
authors.initials: R
authors.lastname: Mantei
authors.forename: Xumiao
authors.initials: X
authors.lastname: Zhao
authors.forename: Vicki L
authors.initials: VL
authors.lastname: Nienaber
authors.forename: Kent
authors.initials: K
authors.lastname: Stewart
authors.forename: Vered
authors.initials: V
authors.lastname: Klinghofer
authors.forename: Jennifer
authors.initials: J
authors.lastname: Bouska
authors.forename: Todd W
authors.initials: TW
authors.lastname: Rockway
authors.forename: Vincent L
authors.initials: VL
authors.lastname: Giranda
mesh_terms: D008958:Models, Molecular; D009281:Naphthalenes / Q000737:chemistry / Q000493:pharmacokinetics*; D015849:Plasminogen Inactivators / Q000737:chemistry / Q000493:pharmacokinetics*; D013379:Substrate Specificity; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*
chemical_list: D009281:Naphthalenes; D015849:Plasminogen Inactivators; C018609:beta-naphthamidine; D014568:Urokinase-Type Plasminogen Activator