2-substitiuted thio- and amino-5,8-dimethoxy-1,4-naphthoquinones as a novel class of Acyl-CoA: cholestrol acyltransferase inhibitors

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Title
2-substitiuted thio- and amino-5,8-dimethoxy-1,4-naphthoquinones as a novel class of Acyl-CoA: cholestrol acyltransferase inhibitors
Author(s)
G N Shen; Jung Ho Choi; K Gajulapati; J H Lee; Young Kook Kim; Mun Chual Rho; S H Jung; Kyeong Lee; S S Han; G Y Song; Y Choi
Bibliographic Citation
Bulletin of Korean Chemical Society, vol. 30, no. 5, pp. 1088-1092
Publication Year
2009
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.
Keyword
naphthoquinonesmast cells, acyl CoACholestrol Acyl Transferase (ACAT)structure-activity
ISSN
0253-2964
Publisher
Wiley
DOI
http://dx.doi.org/10.5012/bkcs.2009.30.5.1088
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Immunoregulatory materials Research Center > 1. Journal Articles
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