title: Ligustrazine derivatives. Part 4: design, synthesis, and biological evaluation of novel ligustrazine-based stilbene derivatives as potential cardiovascular agents.
abstract: A series of novel stilbene derivatives containing ligustrazinyl moiety was designed, synthesized, and assayed for their protective effects on damaged endothelial cells. The results showed that most ligustrazinyl stilbene derivatives exhibited high protective effects on the human umbilical vascular endothelial cells (HUVECs) damaged by hydrogen peroxide in comparison with Ligustrazine. The stilbene derivatives A6, A9, A11, A21, A24, A25, and A27 exhibited high potency with low EC(50) values ranged from 0.0249 μm to 0.0898 mm. Compound A27 displayed EC(50) 0.0249 μm, which is 30,000 times higher than that of Ligustrazine, presenting a most promising lead for further investigation. Structure-activity relationships were briefly discussed.
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, No. 44 Wenhuaxi Road, Jinan, China.
authors.forename: Lijuan
authors.initials: L
authors.lastname: Deng
authors.forename: Xiuli
authors.initials: X
authors.lastname: Guo
authors.forename: Li
authors.initials: L
authors.lastname: Zhai
authors.forename: Yuning
authors.initials: Y
authors.lastname: Song
authors.forename: Hongfei
authors.initials: H
authors.lastname: Chen
authors.forename: Peng
authors.initials: P
authors.lastname: Zhan
authors.forename: Jingde
authors.initials: J
authors.lastname: Wu
authors.forename: Xinyong
authors.initials: X
authors.lastname: Liu
mesh_terms: D002317:Cardiovascular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects / Q000473:pathology; D006801:Humans; D006861:Hydrogen Peroxide / Q000378:metabolism; D018384:Oxidative Stress / Q000187:drug effects; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D002317:Cardiovascular Agents; D011719:Pyrazines; D013267:Stilbenes; D006861:Hydrogen Peroxide; C017953:tetramethylpyrazine