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Synthesis and Nuclear Factor-${kappa}B$ Inhibitory Activities of 6- or 7-Methylchroman-2-carboxylic Acid N-(Substituted) Phenylamides
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  • Synthesis and Nuclear Factor-${kappa}B$ Inhibitory Activities of 6- or 7-Methylchroman-2-carboxylic Acid N-(Substituted) Phenylamides
  • Synthesis and Nuclear Factor-${kappa}B$ Inhibitory Activities of 6- or 7-Methylchroman-2-carboxylic Acid N-(Substituted) Phenylamides
저자명
Kwak. Jae-Hwan,Won. Sun-Woo,Kim. Tae-Jeong,Yi. Won-Hui,Choi. Eun-Hwa,Kim. Seung-Chan,Park. Hyun-Jeong,Roh. Eun-Mi-Ri,Jung. Jae-K
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2009년|32권 2호|pp.167-175 (9 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

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-${kappa}B$ (NF-${kappa}B$) activity were evaluated in lipopolysaccharide (LPS)-stimulated macrophage RAW 264.7 cells. Compounds with substituents such as -H, $-CH_3$, and $-CH_3$ on the phenyl ring were poor inhibitors of NF-${kappa}B$. The most active NF-${kappa}B$ inhibitors contained 4-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 ($IC_{50}$: $20.2-24.0;{mu}M$). These were slightly more potent than a reference compound, KL-1156 (1) ($IC_{50}$: $43.9;{mu}M$).