title: Parallel approach for solution-phase synthesis of 2-quinoxalinol analogues and their inhibition of LPS-induced TNF-alpha release on mouse macrophages in vitro.
abstract: A parallel solution-phase synthesis of 2-quinoxalinol analogues is described. The key step-simultaneous reductions of m-Ar(NO2)2 to m-Ar(NH2)2 was investigated extensively. We obtained preliminary pharmacological activity of those analogues for the inhibition of LPS-induced TNF-alpha release on mouse macrophage in vitro. Two compounds revealed inhibitory activity, with IC50 values of 0.40 microM (7-amino-6-[(3-methoxypropyl)amino]-3-methyl-2-quinoxalinol) and 2.2 microM (7-amino-6-[(3-butoxypropyl)amino]-3-methyl-2-quinoxalinol), respectively.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, P. R. China.
authors.forename: Liang
authors.initials: L
authors.lastname: Zhang
authors.forename: Gang
authors.initials: G
authors.lastname: Liu
authors.forename: Suo-De
authors.initials: SD
authors.lastname: Zhang
authors.forename: Hong-Zhen
authors.initials: HZ
authors.lastname: Yang
authors.forename: Li
authors.initials: L
authors.lastname: Li
authors.forename: Xiang-Hong
authors.initials: XH
authors.lastname: Wu
authors.forename: Junli
authors.initials: J
authors.lastname: Yu
authors.forename: Bin-Bin
authors.initials: BB
authors.lastname: Kou
authors.forename: Song
authors.initials: S
authors.lastname: Xu
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.forename: Gang-Chun
authors.initials: GC
authors.lastname: Sun
authors.forename: Ya-Fei
authors.initials: YF
authors.lastname: Ji
authors.forename: Gui-Fang
authors.initials: GF
authors.lastname: Cheng
mesh_terms: D000818:Animals; D008070:Lipopolysaccharides; D008264:Macrophages; D051379:Mice; D019999:Pharmaceutical Solutions; D012996:Solutions; D014409:Tumor Necrosis Factor-alpha
chemical_list: D008070:Lipopolysaccharides; D019999:Pharmaceutical Solutions; D012996:Solutions; D014409:Tumor Necrosis Factor-alpha