Synthesis Of 2-methoxyestradiol Derivatives And Biological Activity

In this thesis, the reseach progress of bioactivities including anti-tumor and treatment of cardiovascular disease, immunoregulation activation of estradiol and its derivatives and analogues were reviewed. The syntheses of 2- methoxyestradiol (2ME2) and the analogues were also studied.Using 2-methoxyestradiol as the lead compound, the derivatives were designed and synthesized.2ME2 Mannich base derivatives were designed by introducing aminomethyl in the benzene ring.The isomers of 2ME2 Mannich base derivatives were obtained by change the position of methoxy. According to the structures of tamoxife and raloxifene, substitute-aminoalkyloxy derivatives were designed and synthesized. All the 40 compounds have not been reported in literatures yet. The structures of the target compounds were confirmed by 1H-NMR,13C-NMRThe effects of 2-methoxyestradiol and its derivatives of HL-60 cell, were evaluated. The result showed that 2-methoxyestradiol and some derivatives had activities, the activity of D2ME-206 is the best. Some target compounds are under investigation.