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

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Title
Synthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors
Author(s)
K Lee; S H Cho; J H Lee; J Goo; S Y Lee; S K Boovanahalli; S K Yeo; S J Lee; Young Kook Kim; D H Kim; Y Choi; G Y Song
Bibliographic Citation
European Journal of Medicinal Chemistry, vol. 62, pp. 515-525
Publication Year
2013
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.
Keyword
ACAT inhibitorsCellular cholesterolLDLNaphthoquinonesTriglyceridesVLDL
ISSN
0223-5234
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.ejmech.2013.01.020
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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