Synthesis of chroman-2-carboxylic acid N-(substituted)phenylamides and their inhibitory effect on nuclear factor-kappaB (NF-kappaB) activation.

Synthesis of chroman-2-carboxylic acid N-(substituted)phenylamides and their inhibitory effect on nuclear factor-kappaB (NF-kappaB) activation. Research Abstract Details 

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Synthesis of chroman-2-carboxylic acid N-(substituted)phenylamides and their inhibitory effect on nuclear factor-kappaB (NF-kappaB) activation. Abstract Text:

Jae-Hwan Kwak,Sun-Woo Won,Tae-Jeong Kim,Eunmiri Roh,Han-Young Kang,Hyo Won Lee,Jae-Kyung Jung,Bang Yeon Hwang,Youngsoo Kim,Jungsook Cho,Heesoon Lee,

A series of chroman-2-carboxylic acid N-(substituted)phenylamides (2a-s, 3a-j) were synthesized. Their ability to inhibit nuclear factor-kappaB (NF-kappaB) activity was evaluated in lipopolysaccharide (LPS)-stimulated macrophage RAW 264.7 cells and their antioxidant activity was examined. NF-kappaB inhibition by chroman compounds was not related to their antioxidant activity. Compounds with -H, -NO2 monosubstituents and -OCH3, -CF3 disubstituents on the phenyl ring were poor inhibitors of NF-kB activity. Compounds with -CH3, -CF3, -CI monosubstituents or -CI, -CH3 disubstituents exhibited moderate to good NF-kappaB activity inhibition (IC50: 18.2-95.8 microM). The most active NF-kappaB inhibitor, 2s, contained a 4-CI (IC50: 18.2 microM) substituent on the phenyl ring and was slightly more potent than the compound KL-1156 (1) (IC50: 43.9 microM).

Synthesis of chroman-2-carboxylic acid N-(substituted)phenylamides and their inhibitory effect on nuclear factor-kappaB (NF-kappaB) activation. Publishing Authors By Initials

JH Kwak,SW Won,TJ Kim,E Roh,HY Kang,HW Lee,JK Jung,BY Hwang,Y Kim,J Cho,H Lee,

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Synthesis of chroman-2-carboxylic acid N-(substituted)phenylamides and their inhibitory effect on nuclear factor-kappaB (NF-kappaB) activation. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Archives of pharmacal research

VOLUME: 31

Page Numbers: 133-41

Journal Abbreviation: Arch. Pharm. Res.

ISSN: 0253-6269

DAY: 27

MONTH: Feb

YEAR: 2008

Synthesis of chroman-2-carboxylic acid N-(substituted)phenylamides and their inhibitory effect on nuclear factor-kappaB (NF-kappaB) activation. Information

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LANGUAGE: eng

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AFFILIATION: College of Pharmacy, Chungbuk National University, Cheongju 361-763, Korea.

Country: Korea (South)

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MEDLINETA: Arch Pharm Res

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