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2-Substituted Thio- and Amino-5,8-dimethoxy-1,4-naphthoquinones as a Novel Class of Acyl-CoA: Cholestrol Acyltransferase Inhibitors
- Shen, Gui-Nan;
- Choi, Ong Ho;
- Gajulapati, Kondaji;
- Lee, Jee Hyun;
- Kim, Young Kook;
- ... Choi, Yongseok;
- 외 5명
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6초록
A series of 2-alkyl or 2-arylthio-5,8-dimethoxy-1,4-naphthoquinones (2-Thio-DMNQ, 5a-s) and 2-alkylamino-5,8-dimethoxy-1,4-naphthoquinones (2-Amino-DMNQ, 6a-k) was synthesized and evaluated for their ACAT inhibitory activities. Among them, the 2-dodecylthio-DMNQ 51 and 2-isobutylamidoundodecylthio-DMNQ 5r showed the most potent ACAT inhibitory activities with IC50 value of 22.8 and 24.4 mu M, respectively. In a structure-activity relationship study, 2-thio-DMNQs with side chains of carbon number 11 similar to 15 exhibited significant ACAT inhibitory activities.
키워드
Naphthoquinones; Mast cells; Acyl CoA: Cholestrol Acyl Transferase (ACAT); Structure-activity relationship; ATHEROSCLEROSIS; MICE
- 제목
- 2-Substituted Thio- and Amino-5,8-dimethoxy-1,4-naphthoquinones as a Novel Class of Acyl-CoA: Cholestrol Acyltransferase Inhibitors
- 저자
- Shen, Gui-Nan; Choi, Ong Ho; Gajulapati, Kondaji; Lee, Jee Hyun; Kim, Young Kook; Rho, Mun Chal; Jung, Sang-Hun; Lee, Kyeong; Han, Sung Sik; Song, Gyu-Yong; Choi, Yongseok
- 발행일
- 2009-05-20
- 유형
- Article
- 권
- 30
- 호
- 5
- 페이지
- 1088 ~ 1092
- 언어
- ENG
- 출판사
- WILEY-V C H VERLAG GMBH
- 발행국가
- 독일
- 분량
- 5 페이지
- ISSN
- E 1229-5949
P 0253-2964