Synthesis, In Silico and In Vitro Evaluation of Some Flavone Derivatives for Acetylcholinesterase and BACE-1 Inhibitory Activity
2020
Thai-Son Tran | Thanh-Dao Tran | The-Huan Tran | Thanh-Tan Mai | Ngoc-Le Nguyen | Khac-Minh Thai | Minh-Tri Le
Acetylcholinesterase (AChE) and &beta:-secretase (BACE-1) have become attractive therapeutic targets for Alzheimer&rsquo:s disease (AD). Flavones are flavonoid derivatives with various bioactive effects, including AChE and BACE-1 inhibition. In the present work, a series of 14 flavone derivatives was synthesized in relatively high yields (35&ndash:85%). Six of the synthetic flavones (B4, B5, B6, B8, D6 and D7) had completely new structures. The AChE and BACE-1 inhibitory activities were tested, giving pIC50 3.47&ndash:4.59 (AChE) and 4.15&ndash:5.80 (BACE-1). Three compounds (B3, D5 and D6) exhibited the highest biological effects on both AChE and BACE-1. A molecular docking investigation was conducted to explain the experimental results. These molecules could be employed for further studies to discover new structures with dual action on both AChE and BACE-1 that could serve as novel therapies for AD.
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