新型噻二唑腙衍生物的合成、抗癌活性及碳酸酐酶抑制活性

H. E. Bostancı, U. Acar Çevik
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引用次数: 0

摘要

分五步合成了噻二唑腙衍生物的新化合物5a、5b。使用各种光谱方法,如1H NMR、13C NMR和元素分析,来阐明化合物的结构。测试了三种癌症细胞系(MCF7、MDA和HT-29)和一种健康细胞系(L929)合成化合物的细胞毒性活性,以及它们对碳酸酐酶I和II同功酶(hCA I和hCA II)的抑制作用。其中,与标准抑制剂相比,化合物5b表现出显著的CA抑制活性,hCA I的IC50值为27µM,hCA II的IC50为33,46µM。已经发现这些化合物对癌症细胞系无效。此外,发现这些化合物对健康细胞系无毒。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, Anticancer Activity and Carbonic Anhydrase Inhibitory Activity of new Thiadiazole-hydrazone Derivatives
In five steps, new compounds 5a, 5b of thiadiazole-hydrazone derivatives were synthesized. Various spectral methods, such as 1H NMR, 13C NMR, and elemental analyses, were used to clarify the structures of the compounds. Three cancer cell lines (MCF7, MDA, and HT-29) and one healthy cell line (L929) were tested for the cytotoxicity activity of synthetic compounds, as well as their inhibitory action against carbonic anhydrase I and II isoenzymes (hCA I and hCA II). Among them, the compound 5b exhibited remarkable CA inhibitory activities compared to a standard inhibitor with IC50 values at of 27 µM for hCA I and 33,46 µM for hCA II. The compounds have been found to be ineffective against cancer cell lines. Furthermore, the compounds were found to be non-toxic to the healthy cell line.
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