Farnesyloxycoumarins, a new class of squalene-hopene cyclase inhibitors

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• 作者：Cravotto ; Giancarlo ; Balliano ; Gianni ; Robaldo ; Bruna ; Oliaro-Bosso ; Simonetta ; Chimichi ; Stefano ; et. al.
• 关键词：Prenylcoumarins ; Squalene hopene cyclase ; Oxidosqualene cyclase ; Selective epoxydation ; Umbelliprenin
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2004
• 出版时间：April 19, 2004
• 年：2004
• 卷：14
• 期：8
• 页码：1931-1934
• 全文大小：170 K

文摘

A few naturally occurring prenyl- and prenyloxycoumarins 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 μM) and the corresponding 6′,7′-10′,11′ diepoxide (IC₅₀ 1.5 μM) were the most active enzyme inhibitors.