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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

Authors 

G N ShenJung Ho ChoiK GajulapatiJ H LeeYoung Kook KimMun Chual RhoS H JungKyeong LeeS S HanG Y SongY Choi

Publisher 

The Korean Chemical Society

Issue Date 

2009

Citation 

Bulletin of the Korean Chemical Society, vol. 30, no. 5, pp. 1088-1092

Keywords 

naphthoquinonesmast cells, acyl CoACholestrol Acyl Transferase (ACAT)structure-activity

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.

ISSN 

0253-2964

Link 

http://dx.doi.org/10.5012/bkcs.2009.30.5.1088

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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