Structure-based drug design of a novel family of chalcones as PPARα agonists: virtual screening, synthesis, and biological activities in vitro1
文献类型：期刊论文
| 作者 | Xianghua LI; Hanjun ZOU; Anhui WU; Yangliang YE ; Jianhua SHEN
|
| 刊名 | Acta Pharmacologica Sinica
 |
| 出版日期 | 2007 |
| 卷号 | 28期号:12页码:2040 |
| 关键词 | peroxisome proliferator-activated receptors drug design virtual screening |
| ISSN号 | 1671-4083 |
| 英文摘要 | Aim: To design and synthesize a novel class of peroxisome proliferator-activated receptors (PPAR)α agonists, which is obtained by the combination of the classical fibrate "head group", a linker with appropriate length and a chalcone. Methods: Thirty seven compounds were designed and identified employing the virtual screening approach. Six compounds were then selected for synthesis and bioassay according to the virtual screening results, structural similarity, and synthetic complexity. Results: Six new compounds (4b and 4d-h) were synthesized and bioassayed. All were found to be potent PPARα agonists, compound 4 h being the most prominent with a 50% effective concentration value of 0.06 μmol/L. Conclusion: This study provides a promising novel family of chalcones with a potential hypolipidemic effect. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/293910]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Xianghua LI,Hanjun ZOU,Anhui WU,et al. Structure-based drug design of a novel family of chalcones as PPARα agonists: virtual screening, synthesis, and biological activities in vitro1[J]. Acta Pharmacologica Sinica,2007,28(12):2040. |
| APA | Xianghua LI,Hanjun ZOU,Anhui WU,Yangliang YE,&Jianhua SHEN.(2007).Structure-based drug design of a novel family of chalcones as PPARα agonists: virtual screening, synthesis, and biological activities in vitro1.Acta Pharmacologica Sinica,28(12),2040. |
| MLA | Xianghua LI,et al."Structure-based drug design of a novel family of chalcones as PPARα agonists: virtual screening, synthesis, and biological activities in vitro1".Acta Pharmacologica Sinica 28.12(2007):2040. |
入库方式： OAI收割
来源：上海药物研究所
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