26-HYDROXYSQUALENE AND DERIVATIVES - SUBSTRATES AND INHIBITORS FOR SQUALENE EPOXIDASE

被引:13
作者
BAI, M
XIAO, XY
PRESTWICH, GD
机构
[1] Department of Chemistry State, University of New York Stoney Brook
关键词
D O I
10.1016/S0960-894X(00)80258-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
26-Hydroxysqualene (26-HS) was synthesized from squalene and shown to be a potent competitive inhibitor (K(l) = 4-mu-M) of partially-purified pig liver squalene epoxidase (SE). The corresponding aldehyde, amine and diazoacetate derivatives were also evaluated as SE inhibitors. The [H-3]26-HS was converted to a mixture of regioisomeric 2,3-epoxides bearing either a 26-hydroxyl or a 29-hydroxyl group.
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页码:227 / 232
页数:6
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