title: Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.
abstract: The identification of a potent series of IKK-beta selective inhibitors based on an imidazothienopyrazine template and the oral efficacy of one such analog (22j) in the LPS-induced TNF-alpha release mouse model are described.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. makonen.belema@bms.com
authors.forename: Makonen
authors.initials: M
authors.lastname: Belema
authors.forename: Amy
authors.initials: A
authors.lastname: Bunker
authors.forename: Van N
authors.initials: VN
authors.lastname: Nguyen
authors.forename: Francis
authors.initials: F
authors.lastname: Beaulieu
authors.forename: Carl
authors.initials: C
authors.lastname: Ouellet
authors.forename: Yuping
authors.initials: Y
authors.lastname: Qiu
authors.forename: Yunhui
authors.initials: Y
authors.lastname: Zhang
authors.forename: Alain
authors.initials: A
authors.lastname: Martel
authors.forename: James R
authors.initials: JR
authors.lastname: Burke
authors.forename: Kim W
authors.initials: KW
authors.lastname: McIntyre
authors.forename: Mark A
authors.initials: MA
authors.lastname: Pattoli
authors.forename: Connie
authors.initials: C
authors.lastname: Daloisio
authors.forename: Kathleen M
authors.initials: KM
authors.lastname: Gillooly
authors.forename: Wendy J
authors.initials: WJ
authors.lastname: Clarke
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Brassil
authors.forename: F Chris
authors.initials: FC
authors.lastname: Zusi
authors.forename: Dolatrai M
authors.initials: DM
authors.lastname: Vyas
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D051550:I-kappa B Kinase / Q000037:antagonists & inhibitors*; D051379:Mice; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011719:Pyrazines; D051550:I-kappa B Kinase