齐墩果酸C28甲酰胺衍生物的合成及活性研究

Synthesis and Activity of Oleanolic Acid C28 Formamide Derivatives

设计并合成一系列齐墩果酸衍生物,并对其抗肿瘤活性进行研究。以齐墩果酸为起始原料,通过对C-3,C-28位经过氧化,酯化,取代,酯化反应得到目标产物。结果表明:合成1个新型的齐墩果酸甲酰胺衍生物4,目标化合物结构经MS,1H NMR确证,利用MTT比色法选择高表达人肺癌细胞、人胃癌细胞对目标化合物进行初步的体外抗肿瘤活性研究,所测化合物对该种肿瘤细胞的抑制活性均明显强于齐墩果酸,值得进一步研究。

Objective:to design and synthesize a series of oleanolic acid derivatives and study their antitumor activities.Methods:oleanolic acid was used as starting material,and the target product was obtained by oxidation,esterification,substitution and esterification of C-3 and c-28 sites.Results:a novel oleanolic acid formamide derivative 4 was synthesized.The structure of the target compound was confirmed by MS and 1H NMR.Conclusion:the antitumor activities of the compounds are stronger than oleanolic acid,which is worthy of further study.