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目的寻找高效低毒的喜树碱类抗肿瘤新药。方法采用相转移催化法合成了6个喜树碱糖苷衍生物(7~12),经1H NMR,IR和MS分析确证了化合物的结构。采用MTT法考察了所合成的喜树碱糖苷对肿瘤细胞抑制活性,采用分子生物学手段考察了所合成的喜树碱糖苷衍生物对Topo I的抑制活性。结果和结论相转移催化法大大提高了喜树碱糖苷的合成收率,喜树碱糖苷类化合物对肿瘤细胞的体外抑制活性较喜树碱母核显著降低,但仍保持很好的Topo I抑制活性。
Objective To search for high-performance and low-toxicity camptothecin anticancer drugs. Methods Six camptothecin derivatives (7-12) were synthesized by phase transfer catalysis. The structures of the compounds were confirmed by 1H NMR, IR and MS. The inhibitory activity of the synthesized camptothecin glycosides on tumor cells was investigated by MTT method. The inhibitory activity of the synthesized camptothecin derivatives on Topo I was investigated by molecular biology. RESULTS AND CONCLUSIONS Phase transfer catalysis greatly enhanced the yield of camptothecin glycosides, which showed a significant decrease in inhibitory activity on tumor cells in vitro compared with camptothecin, yet maintained good Topo I inhibition active.