|
KMID : 0043320080310020133
|
|
Archives of Pharmacal Research
2008 Volume.31 No. 2 p.133 ~ p.141
|
|
|
Synthesis of Chroman-2-carboxylic Acid N-(substituted)Pheny-lamides and Their Inhibitory Effect on Nuclear Factor-xB (NF-xB) Activation
|
|
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 Young-Soo
Cho Jung-Sook
Lee Hee-soon
|
|
|
Abstract
|
|
|
|
A series of chroman-2-carboxylic acid N-(substituted)phenylamides (2a-s, 3a-j) were synthesized. Their ability to inhibit nuclear Factor-xB (NF-xB)activity was evaluated in lipopolysaccharide (LPS)-stimulated macrophage RAW 264.7 cells and their antioxidant activity was examined. NF-xB inhibition by chroman compounds was not related to their antioxidant activity. Compounds with -H,-NO2 monosubstituents and -OCH3,-CE3,-CI disubstituents on the phenyl ring were poor inhibitors of activity. Compounds with monosubstituents or -CI, -CH3 disubstituents exhibited moderate to good NF-xB activity inhibition (IC50:18.2-95.8μM). The most active NF-xB inhibitor, 2s, contained a 4-CI (IC50:18.2μM) substituent on the phenyl ring and was slightly more potent than the compound KL-1156 (IC50:43.9μM).
|
|
|
KEYWORD
|
|
|
NF-xB, inhibitor, Chroman-2-carboxamide
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|