Inhibition of vertebrate squalene epoxidase by isoprenyl gallates and phenylalkyl gallates

被引：10

作者：

Abe, I ^{[1
]}

Kashiwagi, Y ^{[1
]}

Noguchi, H ^{[1
]}

机构：

[1] Univ Shizuoka, Sch Pharmaceut Sci, Shizuoka 4228526, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(00)00526-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Galloy esters with 'substrate-like' isoprenoid or phenylalkyl side chains were newly synthesized and tested for the enzyme inhibition activities toward recombinant rat squalene epoxidase. Isoprenyl gallates (4-6) showed good inhibition (IC50=1.5-5.1 muM), as potent as previously reported substrate analogues, while phenylalkyl gallates (7-10) were moderate inhibitors of the enzyme (IC50 = 12-61 muM). (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2525 / 2528

页数：4

共 14 条

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