| 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 |
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| 引用本文： | 黄永华,李太华.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[J].合成化学,1999,7(2):198-201. |
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| 作者姓名： | 黄永华 李太华 |
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| 作者单位： | 北京师范大学化学系 |
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| 摘 要： | 合成了５个新的去甲基斑螯素衍生物，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（ＫＢ），结肠直肠癌细胞（ＨＣＴ）和肝癌细胞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、肾和脾均有较高的浓集。
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| 关 键 词： | 去甲基斑螯素 衍生物 斑蝥素 抗癌药 |
Synthesis of Norcantharidin Derivative, Iodine125Labelling and Animal Distribution |
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| Li,TaiHuaHuang,YongHua.Synthesis of Norcantharidin Derivative, Iodine125Labelling and Animal Distribution[J].Chinese Journal of Synthetic Chemistry,1999,7(2):198-201. |
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| Authors: | Li TaiHuaHuang YongHua |
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| Abstract: | 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. |
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| Keywords: | Norcantharidin derivatives Iodine125labelling In vivo distribution Antitumor Carcinoma cell Inhibition |
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