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Synthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors
- Lee, Kyeong;
- Cho, Soo Hyun;
- Lee, Jee Hyun;
- Goo, Jail;
- Lee, Sung Yoon;
- 외 7명
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11초록
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.
키워드
Naphthoquinones; ACAT inhibitors; Cellular cholesterol; Triglycerides; LDL; VLDL; ATHEROSCLEROTIC LESIONS; REDUCES ATHEROSCLEROSIS; IN-VITRO; CL-277,082; PROTEINS; PLASMA
- 제목
- Synthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors
- 저자
- 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
- 발행일
- 2013-04
- 유형
- Article
- 권
- 62
- 페이지
- 515 ~ 525