胆酸酰氧基膦酸酯衍生物的合成及抗肿瘤活性  

Synthesis and antitumor activity of cholic acid-phosphonate derivatives

作　　者：郭深深 代本才[2] 陈瑨[2] 霍萃萌[2] 刘晓莉[2,3] 赵永德[1,2] 

机构地区：[1]河南大学天然药物与免疫工程重点实验室,河南开封475004 [2]河南省科学院化学研究所,河南郑州450002 [3]河南大学化学化工学院,河南开封475004

出　　处：《化学研究》2016年第2期183-188,共6页Chemical Research

摘　　要：以胆酸和亚磷酸酯为原料,在缩合剂二环己基碳二亚胺(DCC)和4-二甲基吡啶(DMAP)的催化下进行酯化反应,合成了10个未见报道的胆酸酰氧基膦酸酯衍生物,所有目标化合物均经过TG,IR,1 H NMR,31P NMR和HRMS对其进行了结构确认.利用MTT法测定了目标化合物的抗肿瘤活性,结果显示:目标化合物4H,4I,4J对人肝癌细胞(HepG2)表现出较好的增殖抑制作用.10cholic acid-phosphonate derivatives based on cholic acid andα-hydroxyphosphonate have been synthesized by using DCC/DMAP condition.These compounds were reported for the first time and confirmed by TG,IR,1 H NMR,31 P NMR and HRMS.And the antitumor activity of the cholic acid derivatives have been measured by MTT assay method.The results showed that the target compounds exhibited certain antitumor activity against HepG2,especially 4H,4I,4J.

关 键 词：胆酸 α-羟基膦酸酯 酯化反应 抗肿瘤活性 

分 类 号：O629.2[理学—有机化学]