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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 30, Number 5
BKCSDE 30(5)
May 20, 2009 

 
Title
2-Substitiuted Thio- and Amino-5,8-dimethoxy-1,4-naphthoquinones as a Novel Class of Acyl-CoA: Cholestrol Acyltransferase Inhibitors
Author
Gui Nan Shen, Jong Ho Choi, Kondaji Gajulapati, Jee Hyun Lee, Young Kook Kim, Mun Chal Rho, Sang Hun Jung, Kyeong Lee, Sung Sik Han, Gyu Yong Song*, Yongseok Choi*
Keywords
Naphthoquinones, Mast cells, Acyl CoA: Cholestrol Acyl Transferase (ACAT), Structure-activity relationship
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 5l and 2-isobutylamidoundodecylthio-DMNQ 5r showed the most potent ACAT inhibitory activities with IC50 value of 22.8 and 24.4 μM, respectively. In a structure-activity relationship study, 2-thio-DMNQs with side chains of carbon number 11 ~ 15 exhibited significant ACAT inhibitory activities.
Page
1088 - 1092
Full Text
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