Detailed Information
Cited 0 time in 
Cited 0 time in 
Cited 0 time in
Metadata Downloads
Synthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors
- Authors
- Lee, Kyeong; Cho, Soo Hyun; Lee, Jee Hyun; Goo, Jail; Lee, Sung Yoon; Boovanahalli, Shanthaveerappa K.; Yeo, Siok Koon; Lee, Sung-Joon; Kim, Young Kook; Kim, Dong Hee; Choi, Yongseok; Song, Gyu-Yong
- Issue Date
- 4월-2013
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- Keywords
- Naphthoquinones; ACAT inhibitors; Cellular cholesterol; Triglycerides; LDL; VLDL
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.62, pp.515 - 525
- Indexed
- SCIE
SCOPUS
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 62
- Start Page
- 515
- End Page
- 525
- ISSN
- 0223-5234
- 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-I, 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 4I and 6j emerged as highly potent inhibitors, exhibiting significantly high inhibitory potencies with IC50 values of 0.44 mu M and 0.6 mu M, respectively. Moreover, compound 4I significantly reduced the accumulation of cellular cholesterol in HepG2 cell lines. (C) 2013 Elsevier Masson SAS. All rights reserved.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - Graduate School > Department of Biotechnology > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.