Farnesyloxycoumarins, a new class of squalene-hopene cyclase inhibitors

被引：26

作者：

Cravotto, G

Balliano, G

Robaldo, B

Oliaro-Bosso, S

Chimichi, S

Boccalini, M

机构：

[1] Univ Turin, Dipartimento Sci & Tecnol Farm, I-10125 Turin, Italy

[2] Univ Florence, Dipartimento Chim Organ U Schiff, I-50019 Sesto Fiorentino, Firenze, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 08期

关键词：

prenylcoumarins; squalene hopene cyclase; oxidosqualene cyclase; selective epoxydation; umbelliprenin;

D O I：

10.1016/j.bmcl.2004.01.085

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A few naturally occurring prenyl- and renyloxycoumarins and several new related synthetic derivatives were evaluated as inhibitors of squalene-hopene cyclase (SHC), a useful model enzyme, to predict their interactions with oxidosqualene cyclase (OSC). Umbelliprenin-10',11'-monoepoxide (IC50 2.5 muM) and the corresponding 6',7'-10', 11' diepoxide (IC50 1.5 muM) were the most active enzyme inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1931 / 1934

页数：4

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