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Structure-Activity Relationship of Chroman-2-carboxylic Acid N-Arylalkylamide Derivatives  

Yi, Wonhui (College of Pharmacy, Chungbuk National University)
Hwang, Yeong-Sik (College of Pharmacy, Chungbuk National University)
Han, Sang-Bae (College of Pharmacy, Chungbuk National University)
Kim, Youngsoo (College of Pharmacy, Chungbuk National University)
Jung, Jae-Kyung (College of Pharmacy, Chungbuk National University)
Lee, Heesoon (College of Pharmacy, Chungbuk National University)
Publication Information
YAKHAK HOEJI / v.57, no.6, 2013 , pp. 426-431 More about this Journal
Abstract
In our previous studies, 6-hydroxy-7-methoxychroman-2-carboxylic acid N-phenylamide (KL-1156) was identified as a good inhibitor of nuclear factor-${\kappa}B$ (NF-${\kappa}B$) activation. In continuation of our study, we describe the structure-activity relationship of chroman derivatives containing N-arylalkyl groups and their NF-${\kappa}B$ 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.
Keywords
nuclear factor-${\kappa}B$; KL-1156; chroman; SAR;
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