Design, synthesis and activity of flavonoids aromatase inhibitors

Abstract

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.