title: Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists.
abstract: We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the majority of these analogs also demonstrated modest selectivity against other alpha(v) integrins such as alpha(v)beta1 and alpha(v)beta6.
authors.affiliation: Department of Chemistry, PfizerGlobal Research and Development, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA. mark.l.boys@pfizer.com
authors.forename: Mark L
authors.initials: ML
authors.lastname: Boys
authors.forename: Lori A
authors.initials: LA
authors.lastname: Schretzman
authors.forename: Nizal S
authors.initials: NS
authors.lastname: Chandrakumar
authors.forename: Michael B
authors.initials: MB
authors.lastname: Tollefson
authors.forename: Scott B
authors.initials: SB
authors.lastname: Mohler
authors.forename: Victoria L
authors.initials: VL
authors.lastname: Downs
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Penning
authors.forename: Mark A
authors.initials: MA
authors.lastname: Russell
authors.forename: John A
authors.initials: JA
authors.lastname: Wendt
authors.forename: Barbara B
authors.initials: BB
authors.lastname: Chen
authors.forename: Heather G
authors.initials: HG
authors.lastname: Stenmark
authors.forename: Hongwei
authors.initials: H
authors.lastname: Wu
authors.forename: Dale P
authors.initials: DP
authors.lastname: Spangler
authors.forename: Michael
authors.initials: M
authors.lastname: Clare
authors.forename: Bipin N
authors.initials: BN
authors.lastname: Desai
authors.forename: Ish K
authors.initials: IK
authors.lastname: Khanna
authors.forename: Maria N
authors.initials: MN
authors.lastname: Nguyen
authors.forename: Tiffany
authors.initials: T
authors.lastname: Duffin
authors.forename: V Wayne
authors.initials: VW
authors.lastname: Engleman
authors.forename: Mary Beth
authors.initials: MB
authors.lastname: Finn
authors.forename: Sandra K
authors.initials: SK
authors.lastname: Freeman
authors.forename: Melanie L
authors.initials: ML
authors.lastname: Hanneke
authors.forename: Jeffery L
authors.initials: JL
authors.lastname: Keene
authors.forename: Jon A
authors.initials: JA
authors.lastname: Klover
authors.forename: G Allen
authors.initials: GA
authors.lastname: Nickols
authors.forename: Maureen A
authors.initials: MA
authors.lastname: Nickols
authors.forename: Christina N
authors.initials: CN
authors.lastname: Steininger
authors.forename: Marisa
authors.initials: M
authors.lastname: Westlin
authors.forename: William
authors.initials: W
authors.lastname: Westlin
authors.forename: Yi X
authors.initials: YX
authors.lastname: Yu
authors.forename: Yaping
authors.initials: Y
authors.lastname: Wang
authors.forename: Christopher R
authors.initials: CR
authors.lastname: Dalton
authors.forename: Sarah A
authors.initials: SA
authors.lastname: Norring
mesh_terms: D000951:Antigens, Neoplasm; D002087:Butyrates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000037:antagonists & inhibitors*; D016023:Integrins / Q000037:antagonists & inhibitors; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D000951:Antigens, Neoplasm; D002087:Butyrates; D039302:Integrin alphaVbeta3; D016023:Integrins; D010069:Oxadiazoles; D019030:Receptors, Vitronectin; C094340:integrin alphavbeta1; C073878:integrin alphavbeta6