크로만-2-카르복실산 N-헤테로아릴아마이드 유도체 합성 및 NF-κB 저해 활성

Synthesis and Inhibitory Activity on NF-κB Activation of Chroman-2-carboxylic Acid N-Heteroarylamide Derivatives

Nuclear factor-κB (NF-κB) 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-κB activation. In this continuous study, we describe the synthesis and NF-κB 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).