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Title 

Synthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors

Authors 

K LeeS H ChoJ H LeeJ GooS Y LeeS K BoovanahalliS K YeoS J LeeYoung Kook KimD H KimY ChoiG Y Song

Publisher 

Elsevier

Issue Date 

2013

Citation 

European Journal of Medicinal Chemistry, vol. 62, no. 0, pp. 515-525

Keywords 

ACAT inhibitorsCellular cholesterolLDLNaphthoquinonesTriglyceridesVLDL

Abstract 

We report a new series of naphthoquinone derivatives as potent ACAT inhibitors, which were obtained through structural variations of previously disclosed lead 1. Several analogs represented by 3i-l, 4k-m, 6a-n, 7a, and 7i demonstrated potent human macrophage ACAT inhibitory activity by a cell-based reporter assay with human HepG2 cell lines. In particular, compounds 4l and 6j emerged as highly potent inhibitors, exhibiting significantly high inhibitory potencies with IC50 values of 0.44 μM and 0.6 μM, respectively. Moreover, compound 4l significantly reduced the accumulation of cellular cholesterol in HepG2 cell lines.

ISSN 

0223-5234

Link 

http://dx.doi.org/10.1016/j.ejmech.2013.01.020

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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