title: Synthesis of indolyl-3-acetonitrile derivatives and their inhibitory effects on nitric oxide and PGE2 productions in LPS-induced RAW 264.7 cells.
abstract: Arvelexin is one of major constituents of Brassica rapa that exerts anti-inflammatory activities. Several indolyl-3-acetonitrile derivatives were synthesized as arvelexin analogs and evaluated for their abilities to inhibit NO and PGE2 productions in LPS-induced RAW 264.7 cells. Of the indolyl-3-acetonitriles synthesized, compound 2k, which possesses a hydroxyl group at C-7 position of the indole ring and an N-methyl substituent, more potently inhibited NO and PGE2 productions and was less cytotoxic than arvelexin on macrophage cells.
authors.affiliation: Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, Seoul 130-701, Republic of Korea.
authors.forename: Tae Hoon
authors.initials: TH
authors.lastname: Kwon
authors.forename: Ik Hwan
authors.initials: IH
authors.lastname: Yoon
authors.forename: Ji-Sun
authors.initials: JS
authors.lastname: Shin
authors.forename: Young Hun
authors.initials: YH
authors.lastname: Lee
authors.forename: Bong Jin
authors.initials: BJ
authors.lastname: Kwon
authors.forename: Kyung-Tae
authors.initials: KT
authors.lastname: Lee
authors.forename: Yong Sup
authors.initials: YS
authors.lastname: Lee
mesh_terms: D000097:Acetonitriles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D015232:Dinoprostone / Q000378:metabolism*; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D008070:Lipopolysaccharides / Q000633:toxicity; D051379:Mice; D009569:Nitric Oxide / Q000378:metabolism*; D000094162:Phytoalexins
chemical_list: D000097:Acetonitriles; D000893:Anti-Inflammatory Agents; D015232:Dinoprostone; D007211:Indoles; D008070:Lipopolysaccharides; D009569:Nitric Oxide; C500823:arvelexin; D000094162:Phytoalexins