薯蓣皂苷元抗肿瘤衍生物的设计与合成(Ⅲ)  

The design and synthesis of diosgenin anti-tumor derivatives(Ⅲ)

作　　者：郑微[1] 蒋红平[1] 吴亚克[1] 范举正[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2011年第2期107-111,共5页West China Journal of Pharmaceutical Sciences

摘　　要：目的设计、合成薯蓣皂苷元衍生物并研究其体外抗肿瘤活性。方法以Autodock 4.0为辅助工具设计化合物,采用酰化和取代的方法制备;用MTT法对人恶性黑色素瘤细胞A375、人肺腺癌细胞A549、人肝癌细胞HepG-2进行体外抗肿瘤活性的试验。结果所制9个新化合物的结构经1HNMR,13CNMR确证。药理结果表明:大部分化合物具有一定的抗肿瘤活性。结论化合物Ⅴ、Ⅶ、Ⅹ有较好的抗肿瘤活性。OBJECTIVE To design and synthesize diosgenin derivatives and investigate their antitumor activity.METHODS Compounds were designed by Autodock 4.0,acylation and substitution reactions were chiefly used to synthesize.Antitumor test was applied against human malignant melanoma A375 cells,human lung adenocarcinoma A549 cells,human hepatoma HepG-2 cells in vitro by MTT assay.RESULTS Structures of the nine new compounds were characterized by 1HNMR,13CNMR.Most compounds showed certain antitumor activity.CONCLUSION The antitumor activity of compounds 5,7,10 were potent as the positive reference substances.

关 键 词：薯蓣皂苷元衍生物 合成 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]