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目的合成薯蓣皂苷元衍生物并进行其体外抗肿瘤活性的研究。方法运用Autodock进行目标分子辅助设计。薯蓣皂苷元通过Mitsunobu反应合成1-(3α-薯蓣皂苷元)-1,2,3-三氮唑和1-(3α-薯蓣皂苷元)-1,2,4-三氮唑两个中间体,再分别与不同的溴代物反应得到一系列的盐。采用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试验。结果共合成了14个化合物,其中有10个为新化合物,结构均经1HNMR、13CNMR鉴定。所测化合物均具一定的抗肿瘤活性。结论化合物Ⅰ、的抗肿瘤活性与阳性对照品相当。
Objective To synthesize diosgenin derivatives and study their antitumor activity in vitro. Methods Autodock is used to design molecular aids. Diosgenin was synthesized by Mitsunobu reaction of two intermediates of 1- (3α-diosgenin) -1,2,3-triazole and 1- (3α-diosgenin) -1,2,4-triazole , And then react with different bromides respectively to obtain a series of salts. The anti-tumor activity of human malignant melanoma A375, human lung adenocarcinoma A549 and human hepatoma HepG-2 were tested by MTT assay. Results A total of 14 compounds were synthesized, of which 10 were new compounds. Their structures were identified by 1HNMR and 13CNMR. The tested compounds have certain anti-tumor activity. Conclusion The antitumor activity of compound Ⅰ and is similar to that of positive control.