title: A new synthesis of fully phosphorylated flavones as potent pancreatic cholesterol esterase inhibitors.
abstract: Five flavones possessing one to four phenolic groups were fully phosphorylated efficiently and the obtained compounds showed excellent pancreatic cholesterol esterase (CEase) inhibitory activities with IC(50) in the nanomolar range, which were much more potent than their parent compounds. The inhibition mechanism and kinetic characterization studies indicate that they are irreversible competitive inhibitors.
authors.affiliation: College of Bioscience and Biotechnology, Hunan Agricultural University, Furong District, Changsha 410428, China.
authors.forename: Guoping
authors.initials: G
authors.lastname: Peng
authors.forename: Yidan
authors.initials: Y
authors.lastname: Du
authors.forename: Yingling
authors.initials: Y
authors.lastname: Wei
authors.forename: Jingming
authors.initials: J
authors.lastname: Tang
authors.forename: Ai-Yun
authors.initials: AY
authors.lastname: Peng
authors.forename: Liqun
authors.initials: L
authors.lastname: Rao
mesh_terms: D002384:Catalysis; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D047309:Flavones / Q000138:chemical synthesis* / Q000494:pharmacology; D007700:Kinetics; D015394:Molecular Structure; D010179:Pancreas / Q000201:enzymology*; D010766:Phosphorylation; D002787:Sterol Esterase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D047309:Flavones; D002787:Sterol Esterase