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Synthesis and Inhibitory Activity on NF-${\kappa}B$ Activation of Chroman-2-carboxylic Acid N-Heteroarylamide Derivatives  

Yi, Won-Hui (College of Pharmacy, Chungbuk National University)
Kwak, Jae-Hwan (College of Pharmacy, Chungbuk National University)
Han, Sang-Bae (College of Pharmacy, Chungbuk National University)
Kim, Young-Soo (College of Pharmacy, Chungbuk National University)
Jung, Jae-Kyung (College of Pharmacy, Chungbuk National University)
Lee, Hee-Soon (College of Pharmacy, Chungbuk National University)
Publication Information
YAKHAK HOEJI / v.56, no.3, 2012 , pp. 186-190 More about this Journal
Abstract
Nuclear factor-${\kappa}B$ (NF-${\kappa}B$) has been considered as one of the major targets for therapeutic agents of diverse human diseases. In the previous studies, 6-hydroxy-7-methoxychroman-2-carboxylic acid N-phenylamide (KL-1156) and chroman-2-carboxylic acid N-(4-chlorophenyl)amide were identified as good inhibitors of NF-${\kappa}B$ activation. In this continuous study, we describe the synthesis and NF-${\kappa}B$ inhibitory activities of chroman derivatives containing N-heteroaryl groups for exploration of SAR (structure-activity relationship). In addition, inhibitory effects of cell proliferation are evaluated against human cancer cell lines (NCI-H23 and PC-3).
Keywords
NF-${\kappa}B$; KL-1156; chroman; SAR;
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