六氢-1H-吡咯并[3,4-d]嘧啶衍生物的合成及抗肿瘤活性

以顺丁烯二酸酐为原料,经过水解、缩合、库尔提斯重排、脱保护得到1-苄基-3-氨基-吡咯烷-4-羧酸甲酯盐酸盐,再与硫脲衍生物缩合得到1-苄基-4-(2-甲酸叔丁酯-3-胍基)吡咯烷-3-羧酸甲酯衍生物,最后经过水解、酯化、脱保护得到六氢-1H-吡咯并3,4-d]嘧啶衍生物,其结构经~1H NMR、~(13)C NMR、ESI-MS和元素分析表征。3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐(MTT)法测试其抗肿瘤活性,实验结果表明,其中化合物9d和9g对肿瘤细胞(Bel-7402)株具有明显的抑制活性。

Synthesis and Antitumor Activity of Hexahydro-1H-pyrrolo [3,4-d] Pyrimidine Derivatives

Using maleic anhydride as the starting material, hexahydro-1H-pyrrolo3,4-d] pyrimidine derivatives were synthesized. The structures of all compounds were characterized by ¹H NMR, ¹³C NMR, ESI-MS and elemental analysis. Their antitumor activities against Bel-740 human liver cancer cells were determined by the 3-(4,5)-dimethylthiahiazo(-z-y1)-3,5-di-phenytetrazoliumromide(MTT) assay. The results indicate that these compounds have a certain inhibitory activity in Bel-740 human liver cancer cells, and the inhibitory activity of compounds 9d and 9g reach the average level.