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

• 영문명: Synthesis and Inhibitory Activity on NF-κB Activation of Chroman-2-carboxylic Acid N-Heteroarylamide Derivatives
• 발행기관: 대한약학회
• 저자명: 이원희(Wonhui Yi) 곽재환(Jae-Hwan Kwak) 한상배(Sang-Bae Han) 김영수(Youngsoo Kim) 정재경(Jae-Kyung Jung) 이희순(Heesoon Lee)
• 간행물 정보: 『약학회지』제56권 제3호 (2012년), 186~190쪽, 전체 5쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2012.06.30

영문 초록

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).

키워드

NF-κB KL-1156 chroman SAR