639517-07-0Relevant articles and documents
Phosphaisocoumarins as a new class of potent inhibitors for pancreatic cholesterol esterase
Li, Baojian,Zhou, Binhua,Lu, Hailiang,Ma, Lin,Peng, Ai-Yun
experimental part, p. 1955 - 1963 (2010/06/20)
Due to the importance of pancreatic cholesterol esterase (CEase) as a potential target in atherosclerosis and for the development of hypocholesterolemic agents, there are increasing interests in designing and synthesizing CEase inhibitors. In the present study, we prepared forty-five isocoumarin phosphorus analogues (i.e., phosphaisocoumarins) and investigated the inhibition of these compounds on the CEase. The results showed that some phosphaisocoumarins could act as potent inhibitors of CEase. The most potent inhibitors, compounds 9d, 10a and 12e give IC50 values of 4.8?μM, 2.3?μM and 1.9?μM, respectively. The inhibition mechanism and kinetic characterization studies indicate that they are reversible competitive inhibitors.
The Synthesis of Phosphaisocoumarins by Cu(I)-Catalyzed Intramolecular Cyclization of o-Ethynylphenylphosphonic Acid Monoesters
Peng, Ai-Yun,Ding, Yi-Xiang
, p. 15006 - 15007 (2007/10/03)
Cu(I)-catalyzed intramolecular cyclization of o-ethynylphenylphosphonic acid monoethyl esters was examined, and a new class of six-membered phosphorus heterocycles was formed with high regioselectivity and good yields. The present reaction is the first ex