Synthesis and biological activity of chalcone derivatives as potent activators of Nrf2

HU Wenyuan; CHEN Jie; JIANG Zhengyu; WANG Yalou; YOU Qidong

doi:10.11665/j.issn.1000-5048.20160606

Journal of China Pharmaceutical University > 2016 > 47(6): 666-672. > DOI: 10.11665/j.issn.1000-5048.20160606

HU Wenyuan, CHEN Jie, JIANG Zhengyu, WANG Yalou, YOU Qidong. Synthesis and biological activity of chalcone derivatives as potent activators of Nrf2[J]. Journal of China Pharmaceutical University, 2016, 47(6): 666-672. DOI: 10.11665/j.issn.1000-5048.20160606

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Synthesis and biological activity of chalcone derivatives as potent activators of Nrf2

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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.
- chalcone,
- Nrf2,
- Keap1,
- ARE,
- inductive activity

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Synthesis and biological activity of chalcone derivatives as potent activators of Nrf2

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