Design, synthesis and activity of flavonoids aromatase inhibitors

2018 1st International Conference on Environment Prevention and Pollution Control Technology

生态环境科学

Geng, Yichao^1,2 ; Liu, Yanchun^1,2 ; Lu, Kui^1,2 ; Zhang, Liming^1,2 ; Zhang, Xiuli^1,2 ; Dai, Yujie^1,2

Key Laboratory of Industrial Fermentation Microbiology, Tianjin University of Science and Technology, Tianjin

300457, China^1

Ministry of Education, College of Bioengineering, Tianjin University of Science and Technology, Tianjin

300457, China^2

关键词: Alkylation reactions;    Aromatase inhibitors;    Breast Cancer;    Clinical use;    High throughput screening;    Inhibition activity;    Inhibitory activity;    Natural products;   

Others  :  https://iopscience.iop.org/article/10.1088/1755-1315/199/3/032062/pdf
DOI  :  10.1088/1755-1315/199/3/032062

学科分类：环境科学（综合）

来源: IOP

【 摘 要 】

Steroidal and non-steroidal aromatase inhibitors target the suppression of estrogen biosynthesis in the treatment of breast cancer. However, in this treatment regime, steroid-type inhibitors may have serious side effects. Therefore, in recent years, researchers have increasingly focused on developing non-steroidal derivatives and undertaken experiments to investigate the potential clinical use of these derivatives. As a kind of non-steroidal inhibitor of natural products, flavonoids have great potential to inhibit the activity of aromatic enzymes. In this study, 10 flavonoids-non-steroidal aromatase inhibitors were synthesized by alkylation reaction and structures were determined by 1HNMR analysis. The inhibitory activity of aromatase was determined by using CYP19/MFC high-throughput screening kit. Then, the effect of substituent on the inhibition activity of aromatic enzymes was summarized. The study could provide basic data and ideas for further searching for a higher activity of flavonoid aromatase inhibitors.