Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.
Fitoterapia. 2024 Oct;178:106151. doi: 10.1016/j.fitote.2024.106151. Epub 2024 Aug 6.
In present study, seventeen α-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 μM 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 α-nitrile substituted guaiazulene-based chalcones offered a promising framework for the further development of new highly efficient drugs.
在本研究中，设计、合成并测试了十七种α-氰基取代的愈创木薁基查耳酮衍生物，包括十二种新化合物，评估其抗病毒、细胞毒性和信号通路活性。所有衍生物均表现出针对流感病毒或单纯疱疹病毒（HSV）的潜在抗病毒活性，7g 经硝基取代后，在 30μM 时对 H1N1 病毒表现出强烈的抑制作用，抑制率为 66.0%，7o 用噻吩取代则表现出对 HSV-1 的强大抑制活性，抑制率为 65.8%。此外，一些化合物对肿瘤细胞和缺氧诱导因子-1（HIF1）信号通路具有抑制作用。这些结果表明，α-氰基取代的愈创木薁基查耳酮提供了一个有前途的框架，可进一步开发高效新药。
