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크로만-2-카르복실산 N-헤테로아릴아마이드 유도체 합성 및 NF-κB 저해 활성
이원희(Wonhui Yi),곽재환(Jae-Hwan Kwak),한상배(Sang-Bae Han),김영수(Youngsoo Kim),정재경(Jae-Kyung Jung),이희순(Heesoon Lee) 대한약학회 2012 약학회지 Vol.56 No.3
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).