Abstract
A series of chroman-2-carboxylic acid N-(substituted)phenylamides (2a-s, 3a-j) were synthesized. Their ability to inhibit nuclear factor-κB (NF-κB) activity was evaluated in lipopolysaccharide (LPS)-stimulated macrophage RAW 264.7 cells and their antioxidant activity was examined. NF-κB inhibition by chroman compounds was not related to their antioxidant activity. Compounds with -H, -NO2 monosubstituents and -OCH 3, -CF3 disubstituents on the phenyl ring were poor inhibitors of NF-kB activity. Compounds with -CH3, -CF3, -Cl monosubstituents or -Cl, -CH3 disubstituents exhibited moderate to good NF-κB activity inhibition (IC50: 18.2-95.8 μM). The most active NF-κB inhibitor, 2s, contained a 4-Cl (IC50: 18.2 μM) substituent on the phenyl ring and was slightly more potent than the compound KL-1156 (1) (IC50: 43.9 μM).
Original language | English (US) |
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Pages (from-to) | 133-141 |
Number of pages | 9 |
Journal | Archives of Pharmacal Research |
Volume | 31 |
Issue number | 2 |
DOIs | |
State | Published - Feb 2008 |
Externally published | Yes |
Bibliographical note
Funding Information:This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD) (The Regional Research Universities Program/Chungbuk BIT Research-Oriented University Consortium).
Keywords
- Chroman-2-carboxamide
- NF-κB inhibitor