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KMID : 0370220130570060426
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Yakhak Hoeji
2013 Volume.57 No. 6 p.426 ~ p.431
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Structure-Activity Relationship of Chroman-2-carboxylic Acid N-Arylalkylamide Derivatives
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Yi Won-Hui
Hwang Yeong-Sik
Han Sang-Bae
Kim Young-Soo
Jung Jae-Kyeong
Lee Hee-Soon
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Abstract
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In our previous studies, 6-hydroxy-7-methoxychroman-2-carboxylic acid N-phenylamide (KL-1156) was identified as a good inhibitor of nuclear factor-κB (NF-κB) activation. In continuation of our study, we describe the structureactivity relationship of chroman derivatives containing N-arylalkyl groups and their NF-κB inhibitory activities. In addition, inhibitory effects of cell proliferation are evaluated against human cancer cell lines (NCI-H23 and PC-3). The most active compounds 3i and 3j contained diphenylethyl and diphenylpropyl side chain on amide nitrogen.
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KEYWORD
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nuclear factor-κB, KL-1156, chroman, SAR
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