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Synthesis and Anticancer Activity of Di(3-thienyl)methanol and Di(3-thienyl)methane

机译:二(3-噻吩基)甲醇和二(3-噻吩基)甲烷的合成及抗癌活性

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摘要

Di(3-thienyl)methanol (>2) and di(3-thienyl)methane (>3) have been synthesized and screened against the T98G (brain cancer) cell line. Treatment induced cell death (MTT and macro-colony assay), growth inhibition, cytogenetic damage (micronuclei formation), were studied as cellular response parameters. Treatment with the compounds enhanced growth inhibition and cell death in a concentration dependent manner in both T98G and HEK (normal) cell lines. At higher concentrations (>20 µg/mL) the cytotoxic effects of the compounds were highly significant. The effect on clonogenic capacity and micronuclei formation observed after treatment of cells. Amongst the compounds, compound >2 exhibited potent activity against T98G brain cancer cells. Despite potent in vitro activity, both compounds exhibited less cytotoxicity against normal human HEK cells at all effective concentrations.
机译:已经合成了二(3-噻吩基)甲醇(> 2 )和二(3-噻吩基)甲烷(> 3 ),并针对T98G(脑癌)细胞系进行了筛选。研究了治疗诱导的细胞死亡(MTT和大菌落测定),生长抑制,细胞遗传学损伤(微核形成)作为细胞反应参数。在T98G和HEK(正常)细胞系中,用化合物处理均以浓度依赖性的方式增强了生长抑制和细胞死亡。在较高浓度(> 20 µg / mL)下,化合物的细胞毒性作用非常显着。细胞处理后观察到的对克隆形成能力和微核形成的影响。在这些化合物中,化合物> 2 对T98G脑癌细胞具有强大的活性。尽管有很强的体外活性,两种化合物在所有有效浓度下对正常人HEK细胞的细胞毒性都较小。

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