A new synthesis of fully phosphorylated flavones as potent pancreatic cholesterol esterase inhibitors

G Peng, Y Du, Y Wei, J Tang, AY Peng… - Organic & Biomolecular …, 2011 - pubs.rsc.org
G Peng, Y Du, Y Wei, J Tang, AY Peng, L Rao
Organic & Biomolecular Chemistry, 2011pubs.rsc.org
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 IC50 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.
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 IC50 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.
The Royal Society of Chemistry
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