Design, synthesis and biological activity of α-nitrile substituted guaiazulene-based chalcone derivatives

被引：0
|
作者：
Zhang, Wenjie [1 ,2 ]
Ma, Zongchen [1 ,2 ]
Han, Xiao [1 ,2 ]
Li, Guoqiang [1 ,2 ]
机构：
[1] Ocean Univ China, Sch Med & Pharm, Key Lab Marine Drugs, Chinese Minist Educ, Qingdao 266003, Peoples R China
[2] Pilot Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao 266237, Peoples R China
来源：
FITOTERAPIA | 2024年 / 178卷
关键词：
Nitrile; Guaiazulene; Chalcone; Antiviral; INHIBITORS;
D O I：
10.1016/j.fitote.2024.106151
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In present study, seventeen alpha-nitrile substituted guaiazulene-based chalcone derivatives including twelve new were designed, synthesized, and assayed for antiviral, cytotoxicity and signal pathway activities. All derivatives showed potential antiviral activity towards influenza virus or herpes simplex virus (HSV), 7 g with the substitution of nitro group showed strong effects towards H1N1 virus at 30 mu M with inhibitory rate of 66.0%, 7o with thiophene exhibited potent anti HSV-1 activities with inhibitory rate of 65.8%. Moreover, several compounds exhibited inhibitory effects on tumor cells and hypoxia-inducible factor-1 (HIF1) signaling pathways. These results showed that alpha-nitrile substituted guaiazulene-based chalcones offered a promising framework for the further development of new highly efficient drugs.
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页数：5
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