Analogues of xanthones- -Chalcones and bis-chalcones as alpha-glucosidase inhibitors and anti-diabetes candidates

作者：Cai, Chao Yun; Rao, Li; Rao, Yong; Guo, Jin Xuan; Xiao, Zhi Zun; Cao, Jing Yu; Huang, Zhi Shu; Wang, Bo^*

来源：European Journal of Medicinal Chemistry, 2017, 130: 51-59.

DOI：10.1016/j.ejmech.2017.02.007

• alpha-glucosidase inhibitors
• Chalcones
• Bis-chalcones
• Noncompetitive

Two series of compounds (chalcones and bis-chalcones) were designed, synthesized, and evaluated as aglucosidase 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 aglucosidase with noncompetitive mechanism. Moreover, most of the hydroxy bis-chalcones exhibit good a-glucosidase inhibitory activities in enzyme test. Inspiringly, bis-chalcones 2g (at 1 mu M concentration) has stronger effect than 1-deoxynojirimycin on reducing the glucose level in HepG-2 cells (human liver cancer cell line).

• 出版日期2017-4-21
• 单位中山大学