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Synthesis of Chroman-2-carboxylic Acid N-(substituted)Pheny-lamides and Their Inhibitory Effect on Nuclear $Factor-{kappa}B$ ($NF-{kappa}B$) Activation
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  • Synthesis of Chroman-2-carboxylic Acid N-(substituted)Pheny-lamides and Their Inhibitory Effect on Nuclear $Factor-{kappa}B$ ($NF-{kappa}B$) Activation
  • Synthesis of Chroman-2-carboxylic Acid N-(substituted)Pheny-lamides and Their Inhibitory Effect on Nuclear $Factor-{kappa}B$ ($NF-{kappa}B$) Activation
저자명
Kwak. Jae-Hwan,Won. Sun-Woo,Kim. Tae-Jeong,Roh. Eun-Mi-Ri,Kang. Han-Young,Lee. Hyo-Won,Jung. Jae-Kyung,Hwang. Bang-Yeon,Kim. You
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2008년|31권 2호|pp.133-141 (9 pages)
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대한약학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

A series of chroman-2-carboxylic acid N-(substituted)phenylamides (2a-s, 3a-j) were synthesized. Their ability to inhibit nuclear $factor-{kappa}B$ ($NF-{kappa}B$) activity was evaluated in lipopolysaccharide (LPS)-stimulated macrophage RAW 264.7 cells and their antioxidant activity was examined. $NF-{kappa}B$ inhibition by chroman compounds was not related to their antioxidant activity. Compounds with -H,$-NO_2$ monosubstituents and $-OCH_3,;-CF_3$ disubstituents on the phenyl ring were poor inhibitors of $NF-{kappa}B$ activity. Compounds with $-CH_3,;-CF_3,;-CI$ monosubstituents or -CI, $-CH_3$ disubstituents exhibited moderate to good $NF-{kappa}B$ activity inhibition $(IC_{50}:;18.2-95.8;{mu}M)$. The most active $NF-{kappa}B$ inhibitor, 2s, contained a 4-CI $(IC_{50}:;18.2;{mu}M)$ substituent on the phenyl ring and was slightly more potent than the compound KL-1156 (1) $(IC_{50}:;43.9;{mu}M)$.