4-氨基-1-吡喃糖基/呋喃糖基-1,3,5-三嗪-2(1H)-硫酮类化合物的设计、合成及抗肿瘤活性

Design,synthesis and anti-tumor activity of 4-amino-1-pyranosyl/ribofuranosyl-1,3,5-triazin-2(1H)-thiones

目的设计并合成4-氨基-1-吡喃糖基/呋喃糖基-1,3,5-三嗪-2(1H)-硫酮类化合物,评价其对人乳腺癌细胞MCF-7和人白血病细胞HL-60的生长抑制活性。方法以呋喃/吡喃糖为起始原料,经6步反应合成目标化合物;以氮杂胞苷为阳性对照药,采用MTT法和台盼蓝染色法测试目标化合物对人乳腺癌细胞MCF-7和人白血病细胞HL-60的生长抑制活性。结果与结论合成12个未见文献报道的化合物,其结构经1H-NMR、MS确证;目标化合物具有中等的细胞生长抑制作用。

Objective To design and synthesize 4-amino-1-pyranosyl/ribofuranosyl-1,3,5-triazin-2（ 1H）-thiones derivatives and evaluate their growth inhibition effect against M CF-7 and HL-60 cancer cells. Methods The target compounds were synthesized in 6 steps starting with furanose / pyranose; and their growth inhibition activity against M CF-7 and HL-60 cancer cell lines were tested by M TT assay,with 5-Azacytidine as the positive control. Results and Conclusion Twelve compounds which had not been reported in literatures were synthesized,and their structures were confirmed by1H-NM R and M S. All of targeted compounds showed moderate growth inhibitory effects comparing with 5-azacytidine.