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KMID : 0370220120560030186
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Yakhak Hoeji
2012 Volume.56 No. 3 p.186 ~ p.190
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Synthesis and Inhibitory Activity on NF- Activation of Chroman-2-carboxylic Acid N-Heteroarylamide Derivatives
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Yi Won-Hui
Kwak Jae-Hwan
Han Sang-Bae
Kim Young-Soo
Jung Jae-Kyung
Lee Hee-Soon
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Abstract
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Nuclear factor- (NF-) 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- activation. In this continuous study, we describe the synthesis and NF- 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).
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KEYWORD
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NF-, KL-1156, chroman, SAR
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