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7-아릴옥시-크로만-2-카복사마이드 유도체들의 합성 및 NF-κB 저해활성
최은화(Eun Hwa Choi),곽재환(Jae-Hwan Kwak),김영수(Youngsoo Kim),이희순(Heesoon Lee),정재경(Jae-Kyung Jung) 대한약학회 2010 약학회지 Vol.54 No.3
Nuclear factor-κB (NF-κB) 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-κB inhibitory agents, we reported that KL-1156 (6-hydroxy-7-methoxychroman-2-carboxylic acid phenylamide) exhibited potent inhibitory activity of NF-κB. For further structure-activity relationship, a series of 7-aryloxy-chroman-2-carboxylamide derivatives were synthesized to explore their inhibitory activities of NF-κB.
N-아릴-3-페닐프로판아마이드 유도체 합성 및 NF-κB 저해 활성
최민호(Minho Choi),김영수(Youngsoo Kim),정재경(Jae-Kyung Jung),이희순(Heesoon Lee) 대한약학회 2015 약학회지 Vol.59 No.2
A series of N-substitutedaryl-3-phenylpropanamide derivatives were synthesized and their inhibitory activities on LPS-induced NF-κB 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.
장재용(Jae-Yong Jang),곽재환(Jae-Hwan Kwak),이희순(Heesoon Lee),정재경(Jae-Kyung Jung) 대한약학회 2011 약학회지 Vol.55 No.3
Synthetic studies directed toward an ortho-fluorination of phenols are described. With eugenol as the test compound, effects of base, fluorination agents, and solvents on ortho-fluorination has been investigated.
메틸크로만-2-카르복실산 N-(이치환)페닐아마이드 유도체의 NF-κB 저해 구조-활성 상관 관계
김태정(Tae-Jeong Kim),곽재환(Jae-Hwan Kwak),김영수(Youngsoo Kim),정재경(Jae-Kyung Jung),이희순(Heesoon Lee) 대한약학회 2011 약학회지 Vol.55 No.2
During the search for a novel compound that can inhibit NF-κB activation, 6-hydroxy-7-methoxychroman-2- carboxylic acid phenyl amide (KL-1156) was identified as a good inhibitor of NF-κB 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-κB are compared with activity of KL-1156 and SAR (structure activity relationship) are explored.
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).
4-카바모일옥시메틸-1-아자안트라퀴논 유도체들의 합성 및 세포독성
이희순,이승일,홍승수,조정숙,김영호 충남대학교 약학대학 의약품개발연구소 1998 藥學論文集 Vol.14 No.-
In the course of developing novel antitumor intercalating agents, we synthesized 4-carbamoyloxymethyl-1-azaanthraquinones 7-12. incorporating the latent alkylating functionality. These compounds were designed to explore the effect of substituent on the nitrogen of carbamate. The target compounds were prepared by hetero Diels-Alder reaction as a key step followed by functionalization of benzylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lne (SNU-354: liver and MCF7: breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). the compounds were less potent than doxorubicin against sensitive cell lines. However, the most active compound 12 was not cross-resisitant with doxorubicin against KB-V-1.