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KMID : 0043320090320020167
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Archives of Pharmacal Research
2009 Volume.32 No. 2 p.167 ~ p.175
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Synthesis and Nuclear Factor-κB Inhibitory Activities of 6- or 7-Methylchroman-2-carboxylic Acid N-(Substituted) Phenylamides
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Lee Hee-Soon
Kwak Jae-Hwan
Kim Young-Soo
Hong Jin-Tae
Jung Jae-Kyeong
Hwang Bang-Yeon
Cho Jung-Sook
Roh Eun-Mi-Ri
Park Hyun-Jeong
Yi Won-Hui
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Abstract
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A series of 6- or 7-methylchroman-2-carboxylic acid N-(substituted) phenylamides (2a-s, 3a-s) were synthesized. Their abilities to inhibit nuclear factor-κB (NF-κB) activity were evaluated in lipopolysaccharide (LPS)-stimulated macrophage RAW 264.7 cells. Compounds with substituents such as -H, -CH3, and -CF3 on the phenyl ring were poor inhibitors of NF-κB. The most active NF-κB inhibitors contained4-Cl (3s) and 4-OMe (3g) in the 7-methylchroman-2-carboxamide derivatives and 2-OH (2b) and 4-Cl(2s) in the 6-methylchroman-2-carboxamide derivatives (IC50: 20.2-24.0 μM). These were slightly more potent than a reference compound, KL-1156 (1) (IC50: 43.9 μM).
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KEYWORD
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NF-κB inhibitor, 6-Methylchroman-2-carboxamide, 7-Methylchroman-2-carboxamide
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