title: Structure-activity relationships of a novel class of Src SH2 inhibitors.
abstract: The structure-activity relationships (SAR) of a novel class of Src SH2 inhibitors are described. Variation at the pY+1 and pY+3 side chain positions using 2,4- and 2,5-substituted thiazoles and 1,2,4-oxadiazoles as scaffolds resulted in inhibitors that bound as well as the standard tetrapeptide Ac-pYEEI-NH2.
authors.affiliation: ARIAD Pharmaceuticals, Inc., Cambridge, Massachusetts 02139-4234, USA. john.buchanan@ariad.com
authors.forename: J L
authors.initials: JL
authors.lastname: Buchanan
authors.forename: C B
authors.initials: CB
authors.lastname: Vu
authors.forename: T J
authors.initials: TJ
authors.lastname: Merry
authors.forename: E G
authors.initials: EG
authors.lastname: Corpuz
authors.forename: S G
authors.initials: SG
authors.lastname: Pradeepan
authors.forename: U N
authors.initials: UN
authors.lastname: Mani
authors.forename: M
authors.initials: M
authors.lastname: Yang
authors.forename: H R
authors.initials: HR
authors.lastname: Plake
authors.forename: V M
authors.initials: VM
authors.lastname: Varkhedkar
authors.forename: B A
authors.initials: BA
authors.lastname: Lynch
authors.forename: I A
authors.initials: IA
authors.lastname: MacNeil
authors.forename: K A
authors.initials: KA
authors.lastname: Loiacono
authors.forename: C L
authors.initials: CL
authors.lastname: Tiong
authors.forename: D A
authors.initials: DA
authors.lastname: Holt
mesh_terms: D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*; D018909:src Homology Domains
chemical_list: D013844:Thiazoles