几种苯丙素苷的合成及抗肿瘤活性  

Synthesis and the antitumor activity of several phenylpropanoids

作　　者：张三奇[1] 顾宜[1] 唐荔[1] 遇苏宁[1] 

机构地区：[1]第四军医大学西京医院药剂科,西安710032

出　　处：《中国药物化学杂志》2004年第2期80-83,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的合成单糖苯丙素苷和糖苷衍生物 ,探讨其抗肿瘤活性。方法以苯乙醇为苷元合成单糖苯丙素苷衍生物 ,采用MTT法测定抗肿瘤活性。结果共合成了 9个新化合物 ,其结构经NMR和MS确证。苯丙素苷 3,5 ,8,9和糖苷 6 ,10 ,11在浓度为 10 -7～ 10 -5mol/L时体外抗肿瘤活性较弱。当浓度大于 10 -5mol/L时 ,糖苷 10和 11则有明显的体外抗肿瘤活性。结论单糖苯丙素苷抗肿瘤活性较弱 ;糖苷抗肿瘤活性与苷元的结构有关。Aim To study the synthesis and the antitumor activity of several monosaccharide phenylpropanoids.Methods Monosaccharide phenylpropanoides and glucoside derivatives were synthesized in several steps from tetraacetyl bromoglucose.The MTT method was employed to test the antitumor activity.Results and Conclusion Four Monosaccharide phenylpropanoides and three glucoside derivatives were synthesized and their structures were confirmed by 1H-NMR and MS.Preliminary pharmacological tests indicated the phenylpropanoids synthesized inhibited week tumor cells.Glycosides 10 and 11 possessed stronger antitumor activity than phenylpropanoids synthesized when the concentrations were more than 10 -5 mol·L -1.

关 键 词：药物化学 制备 化学合成 苯丙素苷 

分 类 号：R914[医药卫生—药物化学]