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硫代卡巴腙及其铂(IV)配合物的合成、光谱表征与真核生物DNA降解

Synthesis, spectral characterization and eukaryotic DNA degradation of thiosemicarbazones and their platinum(IV) complexes.

作者信息

Al-Hazmi G A, El-Metwally N M, El-Gammal O A, El-Asmy A A

机构信息

Chemistry Department, Faculty of Science, Taiz University, Taiz, Yemen.

出版信息

Spectrochim Acta A Mol Biomol Spectrosc. 2008 Jan;69(1):56-61. doi: 10.1016/j.saa.2007.03.010. Epub 2007 Mar 16.

DOI:10.1016/j.saa.2007.03.010
PMID:17500028
Abstract

The condensation products of acetophenone (or its derivatives), salicylaldehyde and o-hydroxy-p-methoxybenzophenone with thiosemicarbazide and ethyl- or phenyl-thiosemicarbazide are the investigated thiosemicarbazones. Their reactions with H(2)PtCl(6) produced Pt(IV) complexes characterized by elemental, thermal, mass, IR and electronic spectral studies. The coordination modes were found mononegative bidentate in the acetophenone derivatives and binegative tridentate in the salicylaldehyde derivatives. The complexes were analyzed thermogravimetrically and found highly stable. Some ligands and their complexes were screened against Sarcina sp. and E. coli using the cup-diffusion technique. [Pt(oHAT)(OH)Cl] shows higher activity against E. coli than the other compounds. The degradation power of the tested compounds on the calf thymus DNA supports their selectivity against bacteria and not against the human or related eukaryotic organisms.

摘要

苯乙酮(或其衍生物)、水杨醛和邻羟基对甲氧基二苯甲酮与氨基硫脲以及乙基或苯基氨基硫脲的缩合产物是所研究的缩氨硫脲。通过元素分析、热分析、质谱分析、红外光谱和电子光谱研究,确定了它们与六氯铂酸(H₂PtCl₆)反应生成的铂(IV)配合物。在苯乙酮衍生物中发现配位模式为单负二齿,在水杨醛衍生物中为双负三齿。通过热重分析对配合物进行分析,发现其具有很高的稳定性。使用杯碟扩散技术,对一些配体及其配合物针对八叠球菌属和大肠杆菌进行了筛选。[Pt(oHAT)(OH)Cl]对大肠杆菌的活性高于其他化合物。测试化合物对小牛胸腺DNA的降解能力支持了它们对细菌具有选择性,而对人类或相关真核生物无选择性的结论。

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