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Synthesis, structural characterization and anti-proliferative activity of thiosemicarbazones.

机译：硫代半氨基甲酮的合成，结构表征和抗增殖活性。

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摘要

Thiosemicarbazones are a class of compounds which have been extensively studied for their anti-proliferative biological properties. The biological properties include antitumor, antibacterial, antiviral and antimalarial, with many diseases studied and reported in the literature. Their mechanism of action is speculated to be through DNA intercalation, Ribonucleotide reductase inhibition, Topoisomerase II inhibition etc. A series of substituted acenaphthenequinone thiosemicarbazones were synthesized and characterized using 1H NMR and mass spectrometry. These were expected to potentially show an inhibition mechanism through DNA intercalation. In this study, a series of &agr;-(N) heterocyclic thiosemicarbazone based on 8-hydroxy-2-quinoline carboxaldehyde and 2-acetylquinoline were synthesized and characterized using 1H NMR. A series of 2-acetylthiazole thiosemicarbazones were characterized using 1H NMR and mass spectrometry. This series of compounds showed two equilibrium solution forms when dissolved in deuterated dimethyl sulfoxide. Their equilibrium constants were calculated based on the integration values obtained from 1H NMR peaks. Palladium complexes of ATZ-dMTSC and ATZ-PTSC were synthesized and characterized using 1H NMR. Some of these synthesized compounds were studied for anti-proliferative activity against Bacteria: Bacillus subtilis G+, Staphylococcus aureus G+, Escherichia coli G-, and Pseudomonas aeruginosa G-. Yeast: Candida albicans, and Saccharomyces cerevisiae, and the mold studied was Aspergillus niger..
机译：硫代氨基咔唑是一类化合物，因其抗增殖生物学特性而被广泛研究。生物学特性包括抗肿瘤，抗菌，抗病毒和抗疟疾，许多疾病已在文献中进行了研究和报道。据推测，它们的作用机理是通过DNA插入，​​核糖核苷酸还原酶抑制，拓扑异构酶II抑制等。合成了一系列取代的ena啶醌硫代半咔唑酮，并使用1H NMR和质谱进行了表征。预期这些可能通过DNA嵌入显示抑制机制。在这项研究中，合成了一系列基于8-羟基-2-喹啉甲醛和2-乙酰基喹啉的α-（N）杂环硫半脲，并使用1H NMR进行了表征。使用1 H NMR和质谱对一系列2-乙酰基噻唑硫代半氨基甲酮进行了表征。当溶于氘代二甲基亚砜中时，该系列化合物显示出两种平衡溶液形式。根据从1H NMR峰获得的积分值计算其平衡常数。合成了ATZ-dMTSC和ATZ-PTSC的钯配合物，并使用1 H NMR进行了表征。研究了其中一些合成的化合物对细菌的抗增殖活性：枯草芽孢杆菌G +，金黄色葡萄球菌G +，大肠杆菌G-和铜绿假单胞菌G-。酵母：白色念珠菌和酿酒酵母，所研究的霉菌是黑曲霉。

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  • 作者

    Tummala, Sri Harsha.;

  • 作者单位

    Tennessee Technological University.;

  • 授予单位 Tennessee Technological University.;
  • 学科 Organic chemistry.;Chemistry.;Analytical chemistry.
  • 学位 M.S.
  • 年度 2012
  • 页码 151 p.
  • 总页数 151
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 地下建筑;
  • 关键词

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