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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。方法以薯蓣皂苷元为原料,与不同的L-氨基酸缩合,合成了6个化合物(Ⅰ~Ⅵ);与1,2,3-三氮唑和1,2,4-三氮唑偶联合成了2个中间体(Ⅶ,Ⅷ);再分别与不同的苄溴化合物反应得到一系列的盐(Ⅸ~Ⅻ)。结果合成的化合物中,除化合物Ⅴ外,其余11个是新化合物。结论所合成的化合物结构经1HNMR、13CNMR确证。采用噻唑蓝(MTT)法测定了部分化合物的体外抗肿瘤活性。所测化合物都有良好的抗肿瘤活性,其中,化合物Ⅵ的抗肿瘤活性与阳性对照1-(3β-薯蓣皂苷元)-3-苄基咪唑溴盐相当。
Objective To design and synthesize diosgenin derivatives and study their anti-tumor activity in vitro. Methods Six compounds (Ⅰ ~ Ⅵ) were synthesized from diosgenin with different L-amino acids. Coupled with 1,2,3-triazole and 1,2,4-triazole Two intermediates (Ⅶ, Ⅷ) were synthesized. A series of salts (IX ~ Ⅻ) were obtained by reaction with different benzyl bromide respectively. Results Among the synthesized compounds, 11 were new compounds besides compound V. Conclusion The structures of the synthesized compounds were confirmed by 1HNMR and 13CNMR. In vitro anti-tumor activity of some compounds was determined by MTT assay. The tested compounds all have good anti-tumor activity. Among them, the antitumor activity of compound VI is comparable to the positive control 1- (3β-diosgenin) -3-benzyl imidazolium bromide salt.