Design,synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208 |
| |
| Authors: | Ping Yu Wenjing Liu Jinghui Ren Yingying Wang Yao Ning Mingqi Huang Xinyi Hu Lili Wei Min Ji Jin Cai |
| |
| Affiliation: | 1. School of Chemistry and Chemical Engineering, Southeast University, Nanjing, Jiangsu 211189, PR China;2. School of Biological Science & Medical Engineering, Southeast University, Nanjing 210096, PR China;3. Suzhou Key Laboratory of Biomaterials and Technologies & Collaborative Innovation Center of Suzhou Nano Science and Technology, Suzhou 215123, PR China |
| |
| Abstract: | Bromodomain-containing protein 4 (BRD4) is a new therapeutic target for the treatment of diseases including cardiovascular diseases, cancer, inflammation and central nervous system (CNS) disorders. In this study, we introduced the pharmacophore of fibrates to a BRD4 inhibitor, RVX-208, to design dual-active hypolipidemic compounds, and found that some of new analogues showed favorable hypolipidemic activities. Synthetic accessibility towards this class of compounds optimized RVX-208 as well as would supply more thoughts on hypolipidemic drugs. |
| |
| Keywords: | Corresponding author at: School of Chemistry and Chemical Engineering, Southeast University, Nanjing, Jiangsu 211189, PR China. RVX-208 BRD4 inhibitor Phenoxyacetic derivatives Dual-active Hyperlipoidemia |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
