title: Synthesis of dihydroxanthone derivatives and evaluation of their inhibitory activity against acetylcholinesterase: unique structural analogs of tacrine based on the BCD-ring of arisugacin.
abstract: A general approach to synthesis of dihydroxanthone derivatives is described here. In vitro evaluation of these dihydroxanthones demonstrated that some derivatives possess moderate anti-cholinesterase activities and better selectivities than tacrine for acetylcholinesterase over butyrylcholinesterase. Structural effects on anti-cholinesterase activities were also examined, and docking experiments were carried out to provide preliminary understandings of these experimental observations.
authors.affiliation: Department of Chemistry, University of Minnesota, Minneapolis 55455, USA.
authors.forename: S J
authors.initials: SJ
authors.lastname: Degen
authors.forename: K L
authors.initials: KL
authors.lastname: Mueller
authors.forename: H C
authors.initials: HC
authors.lastname: Shen
authors.forename: J A
authors.initials: JA
authors.lastname: Mulder
authors.forename: G M
authors.initials: GM
authors.lastname: Golding
authors.forename: L L
authors.initials: LL
authors.lastname: Wei
authors.forename: C A
authors.initials: CA
authors.lastname: Zificsak
authors.forename: A
authors.initials: A
authors.lastname: Neeno-Eckwall
authors.forename: R P
authors.initials: RP
authors.lastname: Hsung
mesh_terms: D000110:Acetylcholinesterase / Q000187:drug effects*; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011714:Pyrans / Q000737:chemistry*; D013619:Tacrine / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D002800:Cholinesterase Inhibitors; D011714:Pyrans; C095353:arisugacin; D013619:Tacrine; D000110:Acetylcholinesterase