Design, synthesis, and anti-inflammatory activity both in vitro and in vivo of new betulinic acid analogues having an enone functionality in ring A

被引：53

作者：

Honda, Tadashi

Liby, Karen T.

Su, Xiaobo

Sundararajan, Chitra

Honda, Yukiko

Suh, Nanjoo

Risingsong, Renee

Williams, Charlotte R.

Royce, Darlene B.

Sporn, Michael B.

Gribble, Gordon W. ^{[1
]}

机构：

[1] Dartmouth Coll, Dept Chem, Hanover, NH 03755 USA

[2] Dartmouth Coll Sch Med, Dept Pharmacol & Toxicol, Hanover, NH 03755 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 24期

关键词：

triterpene; betulinic acid; inhibitors of nitric oxide production; RAW; 264.7; cells; inducer of heme oxygenase-1;

D O I：

10.1016/j.bmcl.2006.09.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Fifteen new betulinic acid analogues were designed, synthesized, and tested for anti-inflammatory activity. Many of these analogues effectively suppress nitric oxide (NO) production in RAW cells stimulated with interferon-gamma. Analogue 10 is highly and orally active in vivo for induction of the anti-inflammatory and cytoprotective enzyme, heme oxygenase-1. (c) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：6306 / 6309

页数：4

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