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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 study their anti-tumor activity in vitro. Methods Autodock 4.0 was used as an aid to design compounds. The compounds were prepared by acylation and substitution. The anti-tumor activity of human malignant melanoma A375, human lung adenocarcinoma A549 and human hepatoma HepG-2 were tested by MTT assay . Results The structures of nine new compounds were confirmed by 1HNMR and 13CNMR. Pharmacological results show that: most of the compounds have some anti-tumor activity. Conclusion Compounds Ⅴ, Ⅶ and Ⅹ have good antitumor activity.