The Synthesis Of Resveratrol Derivatives And Analogues With Biological Activity

In this thesis, the research progress of bioactivities that includes anti-tumor, prevention and treatment of cardiovascular disease, anti-inflammatory, immunoregulation, hormonal regulation and inhibiting the microglia activation of resveratrol derivatives and analogues were reviewed. The synthesis of the resveratrol derivatives and the analogues was also studied.Using resveratrol as the lead compound, the derivatives and analogues were designed and synthesized. To enhance the stability of the target compounds, resveratrol was methylated. Changing the position of the methoxy, other different target compounds were obtained. Referring to the structures of tamoxifen and raloxifene, substituted-aminoalkyloxy derivatives were designed and synthesized. The benzene ring was substituted by quinoline ring, the substituted-quinoline ring analogues were obtained. In this thesis, 22 derivatives and analogues of resveratrol have been designed and synthesized, 12 of them have not been reported in literature. These target compounds were comfirmed by ¹H-NMR, ¹³C-NMR and ESI-MS.The results of the induced apoptosis experiments of resveratrol and some target compounds to NB4 cell showed that some target compounds had excellent induced apoptosis activities, the apoptosis rate being higher than 80.0%.The effects of resveratrol and its substituted-quinoline ring analogues of HL-60 cell, K562 cell, MDA-MB231 cell and MCF-7 cell were evaluated. The result showed that resveratrol and some analogues had good activities. Some target compounds are under investigation.Reported in literature, the resveratrol inhibited the activation of microglia and blocked the receptor signal transduction. The inhibiting microglia activation experiments of resveratrol and some target compounds to NB9 cell are under investigation.