Synthesis and Anticancer Activity of Bis-Thiosemicarbazone Complexes

Muhammad Hamza Ashfaq
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Abstract

In a present review article, relationships were identified between the structure and activity of the bis-thiosemicarbazone ligands and their zinc and copper complexes. These compounds have different substituents at the diimine point and terminal nitrogen of the backbone. All the copper complexes showed distortion in geometry from square planar while all the zinc complexes showed distortion in geometry from square pyramidal. In electrochemistry determination by cyclic voltammetry, all the copper complexes were found quasi-reversible. When the antiproliferative activity was checked against tumor cells, copper complexes showed the greatest activity. It was seen that antiproliferative activity was decreased when hydrophobic moieties were present at diimine points and terminal nitrogen. Zinc complexes showed the lowest antiproliferative activity because they were failed in ligand delivery intracellularly as they were not chaperone. But cobalt showed good activity by successfully delivering the ligand acting as chaperone1. Copper complexes showed more antiproliferative activity as compared to the ligand. In the environment of the tumor, hypoxia was found which decreased the antiproliferative activity of the ligand and its copper complexes. In the present study, it was concluded that this relationship could be helpful in the synthesis of antitumor agents such as bis-thiosemicarbazone and its complexes.
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双硫代氨基脲配合物的合成及抗癌活性研究
本文综述了双硫代氨基脲配体及其锌铜配合物的结构和活性之间的关系。这些化合物在主链的二亚胺点和末端氮上有不同的取代基。所有铜配合物均表现出方形平面的几何畸变,而所有锌配合物均表现出方形金字塔的几何畸变。在循环伏安法的电化学测定中,所有铜配合物都是准可逆的。当对肿瘤细胞进行抗增殖活性检查时,铜配合物显示出最大的活性。当疏水基团存在于二亚胺点和末端氮时,抗增殖活性降低。锌配合物表现出最低的抗增殖活性,因为它们不是伴侣,不能在细胞内传递配体。但钴通过成功递送配体作为伴侣而表现出良好的活性。与配体相比,铜配合物具有更强的抗增殖活性。在肿瘤环境中,发现缺氧降低了配体及其铜配合物的抗增殖活性。本研究认为,这种关系可能有助于双硫代氨基脲及其配合物等抗肿瘤药物的合成。
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