Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester

被引：25

作者：

Wang, Peng ^{[2
]}

Liu, Chuan ^{[2
]}

Sanches, Tino ^{[1
]}

Zhong, Yuan ^{[2
]}

Liu, Bo ^{[2
]}

Xiong, Junlong ^{[2
]}

Neamati, Nouri ^{[1
]}

Zhao, Guisen ^{[2
]}

机构：

[1] Univ So Calif, Sch Pharm, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA

[2] Shandong Univ, Sch Pharmaceut Sci, Jinan 250012, Shandong, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

基金：

中国国家自然科学基金;

关键词：

HIV; Integrase inhibitors; Caffeic acid phenethyl ester; Antiviral; DERIVATIVES; MECHANISM; PEPTIDES; ANALOGS;

D O I：

10.1016/j.bmcl.2009.06.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of nitrogen-containing polyhydroxylated aromatics from caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase inhibitors. Most of these compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in the 3'-end processing and the strand transfer. Their key structure-activity relationship was also discussed. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4574 / 4578

页数：5

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