Structure-activity relationships of 6-hydroxy-7-methoxychroman-2-carboxylic acid N-(substituted)phenylamides as inhibitors of nuclear factor-kB activation

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• 作者：Jae-Hwan Kwak (1)
  Byung Hak Kim (1)
  Jae-Kyung Jung (1)
  Youngsoo Kim (1)
  Jungsook Cho (1) (2)
  Heesoon Lee (1)
  
• 关键词：NF ; kB inhibitor ; Chroman ; 2 ; carboxamdie
• 刊名：Archives of Pharmacal Research
• 出版年：2007
• 出版时间：October 2007
• 年：2007
• 卷：30
• 期：10
• 页码：1210-1215
• 全文大小：525KB
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  13. Umezawa, K. and Chaicharoenpong, C., Molecular design and biological activities of NF-kB inhibitors. / Mol. Cell., 14, 163-67(2002).
  
• 作者单位：Jae-Hwan Kwak (1)
  Byung Hak Kim (1)
  Jae-Kyung Jung (1)
  Youngsoo Kim (1)
  Jungsook Cho (1) (2)
  Heesoon Lee (1)
  
  1. College of Pharmacy, Chungbuk National University, Cheongju, 361-763, Chungbuk, Korea
  2. College of Medicine, Dongguk University, 780-714, Gyeongju, Korea
  
• ISSN：1976-3786

文摘

A series of 6-hydroxy-7-methoxychroman-2-carboxylic acid N-substitutedphenylamides (2a-n) were synthesized and their ability to inhibit nuclear factor-KB activity was evaluated in lipopolysaccharide (LPS)-stimulated macrophage RAW 264.7 cells. While compounds bearing-OH, or -OCH3 substituents were inactive, compounds with -CH3, -CF3, or -CI substituents were potent inhibitors (IC50: 6.0-60.2 μM). The most active compound, 2n, contained a 4-CI substituent on the phenyl ring and was four times more potent than the compound KL-1156.