Synthesis of indolyl-3-acetonitrile derivatives and their inhibitory effects on nitric oxide and PGE2 productions in LPS-induced RAW 264.7 cells

被引：12
|
作者：
Kwon, Tae Hoon [1 ,2 ]
Yoon, Ik Hwan [1 ,2 ]
Shin, Ji-Sun [2 ]
Lee, Young Hun [1 ,2 ]
Kwon, Bong Jin [1 ,2 ]
Lee, Kyung-Tae [1 ,2 ]
Lee, Yong Sup [1 ,2 ]
机构：
[1] Kyung Hee Univ, Dept Life & Nanopharmaceut Sci, Seoul 130701, South Korea
[2] Kyung Hee Univ, Coll Pharm, Dept Pharm, Seoul 130701, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 09期
基金：
新加坡国家研究基金会;
关键词：
Arvelexin; Indole-3-acetonitrile; Nitric oxide; Prostaglandin E-2; Anti-inflammatory; NF-KAPPA-B; PHYTOALEXINS; ROOTS; PHYTOANTICIPINS; EXPRESSION; RAPA;
D O I：
10.1016/j.bmcl.2013.02.114
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Arvelexin is one of major constituents of Brassica rapa that exerts anti-inflammatory activities. Several indolyl-3-acetonitrile derivatives were synthesized as arvelexin analogs and evaluated for their abilities to inhibit NO and PGE(2) productions in LPS-induced RAW 264.7 cells. Of the indolyl-3-acetonitriles synthesized, compound 2k, which possesses a hydroxyl group at C-7 position of the indole ring and an N-methyl substituent, more potently inhibited NO and PGE(2) productions and was less cytotoxic than arvelexin on macrophage cells. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2571 / 2574
页数：4
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