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中文摘要：
目的为了提高DNA甲基转移酶抑制剂氮杂胞苷的稳定性,降低其细胞毒作用,以氮杂胞苷为先导化合物,设计并合成了6-氨基-4-烷基/芳基-1-吡喃糖基-1,3,5-三嗪-2（1H）-酮和4-氨基-6-烷基-1,3,5-三嗪-2-基-1-硫代-吡喃糖苷两类化合物。方法以眯基脲（或眯基硫脲）与原酸酯（或苯甲酸甲酯）为起始原料,经5步反应合成目标化合物;以氮杂胞苷为阳性对照药,采用MTT法评价了目标化合物对人白血病细胞HL-60和人乳腺癌细胞MCF-7的体外抗增殖活性及与全反式维甲酸（all-trans retinoic acid,ATRA）的联合用药情况。结果与讨论合成了16个未见文献报道的化合物,其结构经1H-NMR谱和MS谱确证;与氮杂胞苷相比,目标化合物细胞毒作用均显著降低,具有中等强度的细胞生长抑制作用;吡喃糖/双糖硫苷4-胺基-6-甲基-1,3,5-三嗪-2-基-1-硫代-6＇-去氧-α-L-吡喃甘露糖苷（化合物7g）和ATRA联合用药能增强抗M CF-7增殖活性,有进一步研究的价值。
英文摘要：
Objective To improve the stability and decrease the cytotoxicity of azacytidines as DNA methyltransferase inhibitors, two series of 5-azacytidine analogues including 6-amino-4-alkyl/aryl-1- pyranosyl-1,3, 5-triazin-2 （ 1H ）-ones and 4-amino-6-alkyl-1, 3, 5-triazin-2-yl-l-thio-pyranosides were designed and synthesized. Methods Target compounds were synthesized in 5 steps starting with amidinourea （ or amidinothiourea） and orthoesters （ or methyl benzoate ）. Antiproliferative activities against HL-60 and MCF-7 cell lines were evaluated by alone and in combination with all-trans retinoic acid（ATRA）in vitro by a MTF assay. Results and Conclusion Sixteen compounds were synthesized,and their structures were confLrrned by 1H-NMR and MS. MTF assay showed decreased cytotoxicity, and moderate growth inhibitory effects compared to 5-azacytidine. Compound 7g with pyranosides/disaccharide enhanced the antiproliferative activity against MCF-7 when combined with ATRA. Such phenomenon deserves further investigation.
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