Synthesis and biological activity of chalcone derivatives as potent activators of Nrf2
10.11665/j.issn.1000-5048.20160606
- VernacularTitle:类查尔酮Nrf2激活剂的合成及ARE诱导活性
- Author:
Wenyuan HU
1
;
Jie CHEN
;
Zhengyu JIANG
;
Yalou WANG
;
Qidong YOU
Author Information
1. 中国药科大学〓江苏省药物分子设计与成药性优化重点实验室；药物化学教研室
- Publication Type:Journal Article
- Keywords:
chalcone;
Nrf2;
Keap1;
ARE;
inductive activity
- From:
Journal of China Pharmaceutical University
2016;47(6):666-672
- CountryChina
- Language:Chinese
-
Abstract:
To obtain ARE-Nrf2 potent activators through modifying the structure of the lead compound CPUY191001. 17 compounds were synthesized by aldol condensation, their cytotoxicity were tested using MTT assay, and ARE inductivity of these target compounds were analyzed by luciferase reporter gene assay. The biological evaluation results showed that most synthesized chalcone derivatives nearly had no cytotoxicity, and compounds 2, 3, 10 conducted better activity and in concentration-dependent manner. Compounds 2, 3, 10 are potential agents in the development of anti-inflammatory and chemoprevention, suggesting that compounds 2, 3, 10 are worth for further investigation.
