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곽재환,원선우,정재경,황방연,홍진태,김영수,조정숙,이희순,김태정,이원희,최운화,김성찬,박현정,Eunmiri Roh 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.2
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).