YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Synthesis and Inhibitory Activity on NF-${\kappa}B$ Activation of Chroman-2-carboxylic Acid N-Heteroarylamide Derivatives

크로만-2-카르복실산 N-헤테로아릴아마이드 유도체 합성 및 NF-${\kappa}B$ 저해 활성

  • Received : 2012.05.04
  • Accepted : 2012.05.11
  • Published : 2012.06.30
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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

References

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