title: Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.
abstract: A series of inhibitors of mammalian 15-lipoxygenase based on tryptamine and homotryptamine scaffolds is described. Compounds with aryl substituents at C-2 of the indole core of tryptamine and homotryptamine sulfonamides (e.g., 37a-p) proved to be potent inhibitors of the isolated enzyme. Selected compounds also demonstrated desirable inhibition selectivities over isozymes 5- and P-12-LO.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543, USA. david.weinstein@bms.com
authors.forename: David S
authors.initials: DS
authors.lastname: Weinstein
authors.forename: Wen
authors.initials: W
authors.lastname: Liu
authors.forename: Zhengxiang
authors.initials: Z
authors.lastname: Gu
authors.forename: Charles
authors.initials: C
authors.lastname: Langevine
authors.forename: Khehyong
authors.initials: K
authors.lastname: Ngu
authors.forename: Leena
authors.initials: L
authors.lastname: Fadnis
authors.forename: Donald W
authors.initials: DW
authors.lastname: Combs
authors.forename: Doree
authors.initials: D
authors.lastname: Sitkoff
authors.forename: Saleem
authors.initials: S
authors.lastname: Ahmad
authors.forename: Shaobin
authors.initials: S
authors.lastname: Zhuang
authors.forename: Xing
authors.initials: X
authors.lastname: Chen
authors.forename: Feng-Lai
authors.initials: FL
authors.lastname: Wang
authors.forename: Deborah A
authors.initials: DA
authors.lastname: Loughney
authors.forename: Karnail S
authors.initials: KS
authors.lastname: Atwal
authors.forename: Robert
authors.initials: R
authors.lastname: Zahler
authors.forename: John E
authors.initials: JE
authors.lastname: Macor
authors.forename: Cort S
authors.initials: CS
authors.lastname: Madsen
authors.forename: Natesan
authors.initials: N
authors.lastname: Murugesan
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D016859:Lipoxygenase Inhibitors; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*; D014363:Tryptamines / Q000737:chemistry*
chemical_list: D004791:Enzyme Inhibitors; D016859:Lipoxygenase Inhibitors; D013449:Sulfonamides; D014363:Tryptamines