新型缩氨基硫脲化合物的合成及其抗癌活性的研究

SYNTHESIS AND PRELIMINARY STUDY ON A NEW CLASS ANTI TUMOR AGENTS—CETYTHIOPHENE THIOSEMICARBAZONE

摘要: 合成了 6种 2 乙酰噻吩缩氨基硫脲 ,其中 5种为首次合成的新物质。用红外、质谱和元素分析等方法对合成的 6种化合物进行了指认。化合物的体外抗癌活性表明 ,它们对 3种癌细胞均有一定的抑制作用。用 1 1 1 In标记的 6种化合物的动物试验表明 ,放射性标记物随血液循环没有明显的定向浓集。能否为体内肿瘤细胞所摄取 ,有待进一步研究。

Abstract: Six 2 acetylthiophene TSC have been synthesized and characterized by IR,MC and elemental analysis.Five of them are the first prepared compounds.The anti tumor activities of them have been investigated. The results show that they have high inhibition to all three carcinoma cells (KB cell,HCT 8 cell and Bel 7402 cell). These ligands are labeled with 111 In.The biodistributions of six 111 In ligand complexes in mice are determined.The results show that concentrating of 111 In ligand complexes in blood is not apparent.Further study is needed to see the uptake of 111 In ligand complexes by carinoma cells.