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Design and synthesis of further simplified pyripyropene A based ACAT2 selective inhibitors

文献类型：期刊论文

作者Liu, Yi2; Zhang, Xiaowei3; Zhan, Yang1; Li, Boliang3; Lu, Wei2; Nan, Fajun1
刊名TETRAHEDRON
出版日期2019-03-22
卷号75期号:12页码:1819-1825
关键词Pyripyropene A Acyl-coenzyme A Cholesterol acyltransferase 2 selective inhibitors Simplified structure
ISSN号0040-4020
DOI10.1016/j.tet.2019.01.017
通讯作者Li, Boliang() ; Lu, Wei() ; Nan, Fajun(fjnan@simm.ac.cn)
英文摘要Acyl-coenzyme A: cholesterol acyltransferases (ACATs) play the significant role in the formation of cholesterol esters. One form of this enzyme is ACAT2, which not only regulates the balance of cholesterol metabolism in cells but also participates in the "escape" mechanism of hepatocellular carcinoma (HCC) cells. The natural product pyripyropene A (PPPA) and its analogs are the only chemical ACAT2-specific inhibitors. To develop simpler analogs and endeavor to remove a portion of multichiral centers and enrich a variety of analogs, new PPPA analogs are creatively designed and synthesized based on previous work. Among these new analogs, 7a and 9f show better activity and selective inhibition of ACAT2 compared with PPPA. These results will provide a new future for potential therapeutic use in atherosclerosis and HCC. (C) 2019 Elsevier Ltd. All rights reserved.
WOS关键词COACHOLESTEROL ACYLTRANSFERASE 2 ; ACYL-COENZYME ; CHEMICAL-MODIFICATION ; POTENT ; DERIVATIVES ; COA
资助项目Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020301]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000462418900033
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/290217]  
专题新药研究国家重点实验室
通讯作者Li, Boliang; Lu, Wei; Nan, Fajun
作者单位1.Chinese Acad Sci, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
2.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China
3.Chinese Acad Sci, State Key Lab Mol Biol, Inst Biochem & Cell Biol, Shanghai Inst Biol Sci, Shanghai 200031, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Yi,Zhang, Xiaowei,Zhan, Yang,et al. Design and synthesis of further simplified pyripyropene A based ACAT2 selective inhibitors[J]. TETRAHEDRON,2019,75(12):1819-1825.
APA Liu, Yi,Zhang, Xiaowei,Zhan, Yang,Li, Boliang,Lu, Wei,&Nan, Fajun.(2019).Design and synthesis of further simplified pyripyropene A based ACAT2 selective inhibitors.TETRAHEDRON,75(12),1819-1825.
MLA Liu, Yi,et al."Design and synthesis of further simplified pyripyropene A based ACAT2 selective inhibitors".TETRAHEDRON 75.12(2019):1819-1825.

入库方式： OAI收割

来源：上海药物研究所

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