title: Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties.
abstract: 2,3-Diarylfuro[2,3-b]pyridine-4-amines are a novel class of potent and selective inhibitors of Lck. The discovery, synthesis, and structure activity relationships of this series of inhibitors are reported. The most promising compounds were also profiled to deduce their pharmacokinetic properties.
authors.affiliation: Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA. matmarti@amgen.com
authors.forename: Matthew W
authors.initials: MW
authors.lastname: Martin
authors.forename: John
authors.initials: J
authors.lastname: Newcomb
authors.forename: Joseph J
authors.initials: JJ
authors.lastname: Nunes
authors.forename: Jean E
authors.initials: JE
authors.lastname: Bemis
authors.forename: David C
authors.initials: DC
authors.lastname: McGowan
authors.forename: Ryan D
authors.initials: RD
authors.lastname: White
authors.forename: John L
authors.initials: JL
authors.lastname: Buchanan
authors.forename: Erin F
authors.initials: EF
authors.lastname: DiMauro
authors.forename: Christina
authors.initials: C
authors.lastname: Boucher
authors.forename: Theodore
authors.initials: T
authors.lastname: Faust
authors.forename: Faye
authors.initials: F
authors.lastname: Hsieh
authors.forename: Xin
authors.initials: X
authors.lastname: Huang
authors.forename: Josie H
authors.initials: JH
authors.lastname: Lee
authors.forename: Stephen
authors.initials: S
authors.lastname: Schneider
authors.forename: Susan M
authors.initials: SM
authors.lastname: Turci
authors.forename: Xiaotian
authors.initials: X
authors.lastname: Zhu
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000493:pharmacokinetics; D000818:Animals; D006801:Humans; D020128:Inhibitory Concentration 50; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000037:antagonists & inhibitors*; D010599:Pharmacokinetics; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000493:pharmacokinetics; D011725:Pyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck)