title: Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.
abstract: SAR studies of pyrrolo[1,2-f]triazines as JAK2 inhibitors is presented. Achieving JAK2 inhibition selectively over JAK3 is discussed.
authors.affiliation: Bristol-Myers Squibb Co., Princeton, NJ 08543-4000, USA. lalgudi.harikrishnan@bms.com
authors.forename: Lalgudi S
authors.initials: LS
authors.lastname: Harikrishnan
authors.forename: Muthoni G
authors.initials: MG
authors.lastname: Kamau
authors.forename: Honghe
authors.initials: H
authors.lastname: Wan
authors.forename: Jennifer A
authors.initials: JA
authors.lastname: Inghrim
authors.forename: Kurt
authors.initials: K
authors.lastname: Zimmermann
authors.forename: Xiaopeng
authors.initials: X
authors.lastname: Sang
authors.forename: Harold A
authors.initials: HA
authors.lastname: Mastalerz
authors.forename: Walter L
authors.initials: WL
authors.lastname: Johnson
authors.forename: Guifen
authors.initials: G
authors.lastname: Zhang
authors.forename: Louis J
authors.initials: LJ
authors.lastname: Lombardo
authors.forename: Michael A
authors.initials: MA
authors.lastname: Poss
authors.forename: George L
authors.initials: GL
authors.lastname: Trainor
authors.forename: John S
authors.initials: JS
authors.lastname: Tokarski
authors.forename: Matthew V
authors.initials: MV
authors.lastname: Lorenzi
authors.forename: Dan
authors.initials: D
authors.lastname: You
authors.forename: Marco M
authors.initials: MM
authors.lastname: Gottardis
authors.forename: Kathy F
authors.initials: KF
authors.lastname: Baldwin
authors.forename: Jonathan
authors.initials: J
authors.lastname: Lippy
authors.forename: David S
authors.initials: DS
authors.lastname: Nirschl
authors.forename: Ruhui
authors.initials: R
authors.lastname: Qiu
authors.forename: Arthur V
authors.initials: AV
authors.lastname: Miller
authors.forename: Javed
authors.initials: J
authors.lastname: Khan
authors.forename: John S
authors.initials: JS
authors.lastname: Sack
authors.forename: Ashok V
authors.initials: AV
authors.lastname: Purandare
mesh_terms: D004789:Enzyme Activation / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D053614:Janus Kinase 2 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D053616:Janus Kinase 3 / Q000378:metabolism*; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D011758:Pyrroles; D011759:Pyrrolidines; D014227:Triazines; C543493:pyrrolotriazine-4-one; D053614:Janus Kinase 2; D053616:Janus Kinase 3