title: Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
abstract: The synthesis and characterization of a novel polycyclic azaindole based derivative is disclosed, and its binding to JAK2 is described. The compound is further evaluated for its ability to block the EPO/JAK2 signaling cascade in vitro and in vivo.
authors.affiliation: Vertex Pharmaceuticals Inc., Cambridge, Massachusetts 02139-4242, USA.
authors.forename: Tiansheng
authors.initials: T
authors.lastname: Wang
authors.forename: John P
authors.initials: JP
authors.lastname: Duffy
authors.forename: Jian
authors.initials: J
authors.lastname: Wang
authors.forename: Summer
authors.initials: S
authors.lastname: Halas
authors.forename: Francesco G
authors.initials: FG
authors.lastname: Salituro
authors.forename: Albert C
authors.initials: AC
authors.lastname: Pierce
authors.forename: Harmon J
authors.initials: HJ
authors.lastname: Zuccola
authors.forename: James R
authors.initials: JR
authors.lastname: Black
authors.forename: James K
authors.initials: JK
authors.lastname: Hogan
authors.forename: Scott
authors.initials: S
authors.lastname: Jepson
authors.forename: Dina
authors.initials: D
authors.lastname: Shlyakter
authors.forename: Sudipta
authors.initials: S
authors.lastname: Mahajan
authors.forename: Yong
authors.initials: Y
authors.lastname: Gu
authors.forename: Thomas
authors.initials: T
authors.lastname: Hoock
authors.forename: Mark
authors.initials: M
authors.lastname: Wood
authors.forename: Brinley F
authors.initials: BF
authors.lastname: Furey
authors.forename: J Daniel
authors.initials: JD
authors.lastname: Frantz
authors.forename: Lisa M
authors.initials: LM
authors.lastname: Dauffenbach
authors.forename: Ursula A
authors.initials: UA
authors.lastname: Germann
authors.forename: Bin
authors.initials: B
authors.lastname: Fan
authors.forename: Mark
authors.initials: M
authors.lastname: Namchuk
authors.forename: Youssef L
authors.initials: YL
authors.lastname: Bennani
authors.forename: Mark W
authors.initials: MW
authors.lastname: Ledeboer
mesh_terms: D000818:Animals; D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D004921:Erythropoietin / Q000378:metabolism; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D053614:Janus Kinase 2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D047029:Lactams, Macrocyclic / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D016513:Mice, SCID; D008958:Models, Molecular; D008968:Molecular Conformation; D011487:Protein Conformation; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D001372:Aza Compounds; D007211:Indoles; D047029:Lactams, Macrocyclic; D047428:Protein Kinase Inhibitors; D004921:Erythropoietin; D053614:Janus Kinase 2