5,6-二溴去甲基斑蝥亚胺衍生物的合成及^(125)I标记物在动物体内的分布

Synthesis of 5,6 Dibromo Norcantharidinimide Derivatives,Iodine 125 Labelling and in Animal Distribution

对斑蝥素的结构进行改造，可增强其抗癌活性，降低毒性〔１～３〕．作者参照文献〔４〕合成了两个新的５，６二溴去甲基斑蝥亚胺衍生物（Ⅲａ，Ⅲｂ）（见图１），做了抗癌活性筛选，并用１２５Ｉ对化合物（Ⅲａ）进行了标记，观测了其在动物体内的分布．Ｆｉｇ１Ｓｙ...

The two new 5,6 dibromo norcantharidinimide derivatives (Ⅲa) and (Ⅲb) were prepared.A simple,rapid method was described for the labelling of 5,6 dibromo norcantharidinimide derivatives with 125 I. In this paper,the radiolabelling ratio was 96 9% in \%T\%=80 ℃,pH=6,\%t\%=30 min.Two new 5,6 dibromo norcantharidinimide derivatives (Ⅲa) and (Ⅲb) were tested for the inhibition of the Carcinoma cells.It was shown that the 5,6 dibromo norcantharidinimide derivatives(Ⅲa)to Carcinoma cells(KB,HCT,Bel) had the best antitumor activity,it′s inhibition ratio to KB,HCT,Bel were 45 7%,0,41 7%.The in vivo distribution of 125 I 5,6 dibromo norcantharidinimide derivatives(Ⅲa)in the mouse was studied.It was shown that the high uptake of 125 I 5,6 dibromo norcantharidinimide derivatives(Ⅲa)was found in the liver,lungs and the kidney.