大黄素衍生物的化学合成与抗肿瘤活性

目的设计合成一系列大黄素衍生物,以研究其构效关系.方法以天然产物大黄素为原料,通过不同的方法合成一系列大黄素的衍生物,并且通过MTT法测试它们对KLE细胞株的抗肿瘤活性.结果合成了11个大黄素衍生物并通过元素分析、IR、1H-NMR、13C-NMR和MS确证了它们的结构.活性试验显示某些化合物的活性强于大黄素.结论大黄素类化合物是一类很有希望的肿瘤抑制剂,值得进一步开发研究.

Chemical synthesis and antitumor activities of emodin derivatives

Aim To design and synthesize a series of emodin derivatives in order to investigate their structureactivity relationships. Method Starting from the natural product emodin, a series of emodin derivatives were prepared by using various methods and their antitumor activities were tested against KLE cell line by MTT assay. Results Eleven emodin derivatives were prepared and their structures were confirmed by elementary analysis and IR, ^1H-NMR, ^13C-NMR and MS. Some of them were found to exhibit a cytotoxicity profile more potent than emodin in KLE cell line. Conclusion The derivatives of emodin can be regarded as promising potential antitumor agents and it is worthy of being investigated continually.