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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
- Authors
- 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
- Issue Date
- 20-5월-2009
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- Naphthoquinones; Mast cells; Acyl CoA: Cholestrol Acyl Transferase (ACAT); Structure-activity relationship
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.30, no.5, pp.1088 - 1092
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 30
- Number
- 5
- Start Page
- 1088
- End Page
- 1092
- ISSN
- 0253-2964
- Abstract
- 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.
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