Abstract
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.
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Kwak, JH., Kim, B.H., Jung, JK. et al. Structure-activity relationships of 6-hydroxy-7-methoxychroman-2-carboxylic acid N-(substituted)phenylamides as inhibitors of nuclear factor-kB activation. Arch. Pharm. Res. 30, 1210–1215 (2007). https://doi.org/10.1007/BF02980261
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DOI: https://doi.org/10.1007/BF02980261