5-氮杂-5'-脱氧胞苷的合成工艺优化及其对SKOV3作用  

Study on synthesis and activity of 5-Aza-5′-deoxycytidine on SKOV3

作　　者：李飞龙[1] 詹迪迪[1] 李俊[1] 汤文建[1] 金涌[1] 吕雄文[1] 石静波[1] 黄艳[1] 

机构地区：[1]安徽医科大学药学院,合肥230032

出　　处：《安徽医科大学学报》2011年第9期901-904,共4页Acta Universitatis Medicinalis Anhui

基　　金：安徽省科技攻关项目(编号:06013134B);安徽高校省级自然科学研究项目(编号:KJ2008B171)

摘　　要：目的研究优化5-氮杂-5'-脱氧胞苷(5A5DC)的合成工艺,并观察其对卵巢癌细胞SKOV3的作用。方法通过正交设计比较在Hilbert-Johnson偶联反应中不同Lewis酸、催化剂对合成5A5DC的影响;通过绘制细胞生长曲线及四甲基偶氮唑蓝(MTT)还原检测,观察不同浓度5A5DC对体外培养卵巢癌细胞株SKOV3的作用。结果当以无水SnCl4为催化剂、1,2-二氯乙烷为Lewis酸时,5A5DC的收率最高。以双氰胺计,总收率为31%;5A5DC呈浓度依赖抑制SKOV3细胞增殖,以200μmol/L抑制作用较强。结论本研究优化了5A5DC的合成工艺,5A5DC对SKOV3有一定的增殖抑制作用。Objective To study the synthesis of 5-Aza-5′-deoxycytidine（5A5DC）,and observe the inhibition of proliferation in ovarian cancer cell of SKOV3.Methods The effect of different Lewis acid catalysts in Hilbert-Johnson couple reaction were discussed and the orthogonal experiment was applied to optimize.The inhibition of proliferation of human ovary cancer cell line SKOV3 with different concentration 5A5DC in vitro was observed by curve of cell growth and MTT reduction assay.Results The total yield was 31 % under the condition of SnCl4 as the catalyst.The proliferation of SKOV3 was inhibited in a does-dependent manner after treatment with 5A5DC,and the concentration of 200 μmol/L was the strongest inhibitory effect.Conclusion The synthesis of 5A5DC has been optimized,and it can inhibit the proliferation of SKOV3 in some degree.

关 键 词：脱氧胞苷/类似物和衍生物 药物筛选实验 抗肿瘤 DNA甲基化 卵巢肿瘤 

分 类 号：R739.31[医药卫生—肿瘤] R914.5[医药卫生—临床医学]