• 약학회지
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• 제55권2호
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• pp.154-159
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• 2011

During the search for a novel compound that can inhibit NF-${\kappa}B$ activation, 6-hydroxy-7-methoxychroman-2-carboxylic acid phenyl amide (KL-1156) was identified as a good inhibitor of NF-${\kappa}B$ activation. In the present study, we describe the synthesis of methylchroman-2-carboxylic acid N-(disubstituted)phenylamide derivatives (1 and 2 serieses). In addition, their inhibitory effects of NF-${\kappa}B$ are compared with activity of KL-1156 and SAR (structure activity relationship) are explored.

• 약학회지
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• 제54권3호
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• pp.200-204
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• 2010

Nuclear factor-${\kappa}B$ (NF-${\kappa}B$) plays critical roles in physiological and pathological processes such as immune function, cellular growth, homeostasis, apoptosis, and inflammation. As part of our ongoing efforts to develop novel NF-${\kappa}B$ inhibitory agents, we reported that KL-1156 (6-hydroxy-7-methoxychroman-2-carboxylic acid phenylamide) exhibited potent inhibitory activity of NF-${\kappa}B$. For further structure-activity relationship, a series of 7-aryloxy-chroman-2-carboxylamide derivatives were synthesized to explore their inhibitory activities of NF-${\kappa}B$.

• 약학회지
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• 제57권6호
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• pp.426-431
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• 2013

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.

• 약학회지
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• 제59권2호
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• pp.55-58
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• 2015

A series of N-substitutedaryl-3-phenylpropanamide derivatives were synthesized and their inhibitory activities on LPS-induced NF-$1{\kappa}B$ transcriptional activity on RAW 264.7 cells were evaluated. Cl substituted derivatives (1e, 1f) have shown more potent activities than parent hit compound KL-1156.

• 약학회지
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• 제56권3호
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• pp.186-190
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• 2012

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).