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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Authors: | Jae-Hwan Kwak Byung Hak Kim Jae-Kyung Jung Youngsoo Kim Jungsook Cho Heesoon Lee |
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Institution: | College of Pharmacy, Chungbuk National University, Cheongiu 361-763, Korea. |
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Abstract: | A series of 6-hydroxy-7-methoxychroman-2-carboxylic acid N-substitutedphenylamides (2a-n) were synthesized and their ability to inhibit nuclear factor-kappaB 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 microM). 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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Keywords: | NF-kB inhibitor Chroman-2-carboxamdie |
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