新型2-(2-((1h -吲哚-5基)亚甲基)-肼基)-噻唑衍生物的细胞毒性和抗氧化潜力

A. Grozav, Ioana Porumb, L. Gaina, L. Filip, D. Hanganu
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引用次数: 44

摘要

研究了新合成的2-(2-((1h -吲哚-5基)亚甲基)肼基)噻唑衍生物对肝癌细胞株A2780和HeLa的体外细胞毒性。报道了2-(2-(1h -吲哚-5-基)亚甲基肼基)-4-甲基噻唑(1)和2-(2-(1h -吲哚-5-基)亚甲基肼基)-4-苯基噻唑(3)对A2780 [IC50: 11.6 μM(1)和12.4 μM(3)]和HeLa [IC50: 22.4 μM(1)和19.4μM(3)]细胞株具有显著的细胞毒活性。采用DPPH自由基或Fe (TPTZ)3+络合物分光光度法和EPR光谱法对化合物1和3的抗氧化能力进行了评价,结果表明化合物1和3对A2780和HeLa细胞株具有显著的抗氧化活性,同时具有细胞毒作用。此外,基于理论量子化学计算,本研究分析了氢萃取吲哚肼噻唑类化合物与自由基反应的化学选择性。
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Cytotoxicity and Antioxidant Potential of Novel 2-(2-((1H-indol-5yl)methylene)-hydrazinyl)-thiazole Derivatives
Newly synthesized 2-(2-((1H-indol-5yl)methylene)-hydrazinyl)-thiazole derivatives were evaluated for their in vitro cytotoxicity on two carcinoma cell lines A2780 and HeLa. Significant cytotoxic activity for 2-(2-((1H-indol-5-yl)methylene)hydrazinyl)-4-methylthiazole (1) and 2-(2-((1H-indol-5-yl)methylene)hydrazinyl)-4-phenylthiazole (3), on both A2780 [IC50: 11.6 μM (1), and 12.4 μM (3)] and HeLa [IC50: 22.4 μM (1) and 19.4μM (3)] cell lines is reported. Their antioxidant potential was evaluated by spectrophotometric method, using DPPH radical or Fe (TPTZ)3+ complex, and EPR spectroscopy, therefore the compounds 1 and 3 showed remarkable antioxidant activity simultaneously with a cytotoxic effect on A2780 and HeLa cell lines. Furthermore, based on theoretical quantum chemical calculation, the present study analyzed the chemoselectivity of the hydrogen extraction from the indolyl-hydrazinil-thiazoles in reaction with free radicals.
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