Design, synthesis and biological evaluation of 3′-benzylated analogs of 3′-epi-neoponkoranol as potent α-glucosidase inhibitors
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- 作者：Dan Liua ; b ; 1 ; Weigang Hea ; b ; 1 ; Zihao Wanga ; b ; Long Liua ; b ; Chengqian Wanga ; b ; Chenxi Zhanga ; b ; Chengcheng Wanga ; c ; Yuxuan Wanga ; c ; Genzoh Tanabed ; Osamu Muraokad ; Xiaoming Wua ; b ; Liang Wua ; c ; wul2004@hotmail.com" class="auth_mail" title="E-mail the corresponding author ; Weijia Xiea ; b ; weijiaxie@cpu.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：α-glucosidase inhibitor ; Neoponkoranol ; Salacia ; Structural modification ; Molecular docking
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：3 March 2016
- 年：2016
- 卷：110
- 期：Complete
- 页码：224-236
- 全文大小：882 K
文摘
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Analogs of 3′-epi-neoponkoranol with 3′-substituents were synthesized.
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Generally, incorporation of ortho-substituted benzyl group is preferred.
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10i showed 10-fold sucrase inhibitory potency relative to Acarbose.
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Docking studies on 10i with ntMGAM presented a new binding mode.
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Cytotoxicity evaluation showed a high level of safety profile of synthesized sulfonium salts.