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KMID : 0043320070300101210
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Archives of Pharmacal Research
2007 Volume.30 No. 10 p.1210 ~ p.1215
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Structure-Activity Relationships of 6-Hydroxy-7-methoxychroman-2-carboxylic acid N-(substituted)phenylamides as Inhibitors of Nuclear Factor-κB Activation
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Kwak Jae-Hwan
Kim Byung-Hak
Jung Jae-Kyung
Kim Young-Soo
Cho Jung-Sook
Lee Hee-Soon
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Abstract
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A series of 6-hydroxy-7-methoxychroman-2-carboxylic acid N-substitutedphenylamides (2a-n) were synthesized and their ability to inhibit nuclear factor-κB 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 -Cl substituents were potent inhibitors (IC50: 6.0-60.2 μM). The most active compound, 2n, contained a 4-Cl substituent on the phenyl ring and was four times more potent than the compound KL-1156
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KEYWORD
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NF-κB inhibitor, Chroman-2-carboxamdie
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