【作者】 王国永；

【导师】 林森；

【作者基本信息】 南昌大学 ， 有机化学， 2006， 硕士

【摘要】 癌症已严重影响了人类的健康，人们正在寻找预防和治疗癌症的新药。大量的研究表明二烃基锡化合物具有一定的抗癌活性。在药物分子中，用硅原子对碳原子进行等电排置换后得到的药物称之为硅药，其特点是其原有药效可以保留，并有可能降低其毒性。为了系统的研究有机锡化合物的构效关系，本文以三甲基氯硅烷和三苯基氯化锡等为原料，制备了三个含硅二烃基锡卤化物，合成了三个含硅二烃基锡二芳香酸酯和三个含硅二烃基锡邻菲罗啉配合物。 R=Me₃SiCH₂，Bu，Ph X=Br，Cl 通过元素分析、红外、核磁共振、X-单晶衍射等手段对上述化合物进行了结构表征。测试结果表明含硅二烃基锡二芳香酸酯的中心锡原子与羰基上的氧配位，中心锡原子为六配位的扭曲八面体构型，二烃基锡邻菲罗啉配合物的中心锡原子与氮原子配位形成六配位的化合物。 部分化合物的生物活性测试结果表明，该类化合物对宫颈癌（Hela）和肺癌（SPC-A-1）都有较好的体外抑制率。 本文对一系列新的具有生物活性含硅二烃基锡化合物的初步研究，丰富了有机锡化学的内容，为研究开发安全高效的有机锡药物作了一些探索性的工作。更多还原

【Abstract】 The health of human being has been harmed by cancer. People are seeking new medicine to defend and completely cure cancer. Lots of research works showed that dialkyltin compounds have obvious antitumour activity. In drug molecule whose certain C atom was substituted by a silicon atom was called silicon drug, the effect of the drug will be reserved and the toxicity be reduced. In order to study systemically the relation between structure and effect of organotin, three diorganotin nitrobenzatolates and threeorganotin phenanthroline complexes containing silicon were synthesized in this paper.Their structure were characterized by elemental analysis、 IR、 ¹H-NMR、 ¹³C-NMR 、 X-ray diffraction. The results indicated that the Sn atom of all complexes is in a six-coordinated distorted octahedron.The preliminary bioassay tests showed that some complexes have a good antitumour activity in vitro against Hela and SPC-A-1 tumour cells.This preliminary research on a series of novel silicon-containing diorganotin compounds with biological activities may enrich the study of organotin chemistry, and provide scientific basis for the exploitation of high-safety and high-efficiency organotin organotin pharmaceuticals.更多还原