去甲基斑蝥素衍生物的合成,碘-125标记及在动物体内的分布  

Synthesis of Norcantharidin Derivative, Iodine125Labelling and Animal Distribution

作　　者：黄永华[1] 李太华[1] 

机构地区：[1]北京师范大学化学系

出　　处：《合成化学》1999年第2期198-201,共4页Chinese Journal of Synthetic Chemistry

摘　　要：合成了５个新的去甲基斑蝥素衍生物，并用碘－１２５对其中之一进行了标记，在Ｔ＝８０℃，ｐＨ＝６，ｔ＝３０ｍｉｎ时标记率可达９５．４％。５个新化合物对口腔上皮癌细胞（ＫＢ），结肠直肠癌细胞（ＨＣＴ）和肝癌细胞（Ｂｅｌ）均有一定的抑制作用，被标记的化合物的抑制率最高，分别为４１．７％，１０．０％和６０．０６％。其在小白鼠体内的心、肝、肺。Five new norcantharidin derivatives were prepared and their inhibition of the carcinoma cell was tested. All the derivatives shown a certain antitumor activity to carcinoma cells(KB,HCT,Bel). A simple and rapid method for labelling one of them was described with I125 and its in vivo distribution of the labelling in mouse was studied, showing a high uptake in the heart, liver, lung, spleen and kidney.

关 键 词：去甲基斑螯素 衍生物 斑蝥素 抗癌药 

分 类 号：TQ463.5[化学工程—制药化工]