European Journal of Medicinal Chemistry p. 51 - 59 (2017)
Update date:2022-07-29
Topics:
Cai, Chao-Yun
Rao, Li
Rao, Yong
Guo, Jin-Xuan
Xiao, Zhi-Zun
Cao, Jing-Yu
Huang, Zhi-Shu
Wang, Bo
Two series of compounds (chalcones and bis-chalcones) were designed, synthesized, and evaluated as α-glucosidase inhibitors (AGIs) with 1-deoxynojirimycin as positive control in vitro. Most of the compounds with two or four hydroxyl groups showed better inhibitory activities than 1-deoxynojirimycin towards α-glucosidase with noncompetitive mechanism. Moreover, most of the hydroxy bis-chalcones exhibit good α-glucosidase inhibitory activities in enzyme test. Inspiringly, bis-chalcones 2g (at 1 μM concentration) has stronger effect than 1-deoxynojirimycin on reducing the glucose level in HepG-2 cells (human liver cancer cell line).
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