5′-脱氧-5′-取代嘧啶氨基核苷类似物的合成及抗肿瘤活性  

Synthesis and anticancer activity of novel pyrimidinyl groups modified ribonucleosides

作　　者：李金梅[1] 闫新豪[2] 王克让[2] 李小六[2] 

机构地区：[1]保定市第一中心医院病理科,河北保定071000 [2]河北大学化学与环境科学学院,河北省化学生物学重点实验室,河北保定071002

出　　处：《河北大学学报（自然科学版）》2014年第4期393-397,共5页Journal of Hebei University(Natural Science Edition)

基　　金：国家自然科学基金资助项目(21172051);河北省自然科学基金资助项目(B2012201041)

摘　　要：通过微波促进的一锅法反应合成了一系列C-5′羟基取代的嘧啶基核苷类衍生物,化合物结构经NMR和HRMS等表征.利用MTT法研究了合成化合物的抗肿瘤活性,二甲氨基修饰的嘧啶基5-甲基尿苷衍生物3a和肌苷衍生物4a显示了好的活性,IC50值分别为10.73和10.99μmol/L.而合成的其他核苷类衍生物在测试的细胞株中没有活性,说明环状氨基修饰的嘧啶基显著降低合成的核苷类衍生物的活性.A series of novel ribonucleosides with C-5′OH replaced by different pyrimidinyl groups were synthesized,which were fully characterized by NMR and HRMS analyses.Furthermore,their anticancer activities in vitro were preliminarily evaluated.Compounds 3aand 4awith dimethylamino modified pyrimidinyl group exhibited cytotoxic activity against A549 cell line with the IC50 values of 10.73and10.99μmol/L,respectively.Moreover,the other ribonuleosides with morpholinyl and piperidyl groups conjugates showed no anticancer activity in the test cell lines,indicated that cyclic amino groups remarkably influenced the anticancer activity of the ribonuleoside derivatives.

关 键 词：核苷 嘧啶基 抗肿瘤 微波促进 

分 类 号：O621.3[理学—有机化学]