【作者】 付志飞；

【导师】 林森；

【作者基本信息】 南昌大学 ， 有机化学， 2005， 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,混合二烃基锡化合物由于含有两个不同的烃基具有更广泛的抗癌活性。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,合成了11个新的含硅混合二烃基锡二芳香酸酯和3个新的二烃基锡Schiff碱配合物。 （1） （Me₃SiCH₂）PhSn（OCOAr）₂ 通过元素分析、红外、紫外、荧光、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。测试结果表明含硅混合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Schiff碱配合物的中心锡原子与氮原子配位形成五配位的化合物。 部分含硅混合二烃基锡二芳香酸酯及Ph（Me₃SiCH₂）SnBr₂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。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, and the activity of mixed diorganotin compounds are more extensive because of two different alkyl. 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, eleven Phenyl（trimethylsilylmethyl）tin Arylcarboxylates and three containing silicon organotin complexes were synthesized in this paper.（1）（Me₃SiCH₂）PhSn（OCOAr）₂Their structure were characterized by elemental analysis、 IR、 UV、 ¹H-NMR、 ¹³C-NMR、 X-ray diffraction. The results indicated that the Sn atom of Phenyl（trimethylsilylmethyl）tin Arylcarboxylates is in a six-coordinated distorted octahedron, while the Sn atom of organotin complexes is in a five-coordinated trigonal bipyramind.The preliminary bioassay tests showed that Phenyl（trirnethylsilylmethyl）tin Arylcarboxylates and Phenyl（trimethylsilylmethyl）tin bis（bromide） have a good antitumour activity in vitro against Hela and SPC-A-1 tumour cells.更多还原