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首页> 外文期刊>RSC Advances >Novel 3-substituted fluorine imidazolium/triazolium salt derivatives: synthesis and antitumor activity
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Novel 3-substituted fluorine imidazolium/triazolium salt derivatives: synthesis and antitumor activity

机译：新型的3-取代的氟咪唑鎓/三唑鎓盐衍生物：合成和抗肿瘤活性

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摘要

A series of novel (+/-)-3-substituted fluorene-imidazolium/triazolium salt derivatives has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of 2-methyl-benzimidazole or 5,6-dimethyl-benzimidazole rings and substitution of the imidazolyl/triazolyl3/4-position with a naphthylacyl or 4-methoxyphenacyl group were important for modulating cytotoxic activity. Compounds 37 and 42 were found to be the most potent derivatives with IC50 values of 0.51-2.51 mu M and exhibited cytotoxic activities selectively against myeloid leukaemia (HL-60), liver carcinoma (SMMC-7721) and lung carcinoma (A549). Compound 37 can remarkably induce the G2/M phase cell cycle arrest and apoptosis in SMMC-7721 cells. Additionally, compound 30 exhibited selective cytotoxicity to some extent between cancer cells (A549) and normal cells (BEAS-2B).
机译：已经制备了一系列新颖的（+/-）-3-取代的芴-咪唑鎓/三唑鎓盐衍生物，并在体外针对一组人类肿瘤细胞系进行了评估。结果表明2-甲基-苯并咪唑环或5,6-二甲基-苯并咪唑环的存在以及用萘甲酰基或4-甲氧基苯甲酰基取代咪唑基/三唑基3 / 4-位对于调节细胞毒性活性是重要的。发现化合物37和42是最有效的衍生物，IC50值为0.51-2.51μM，并且选择性地表现出针对髓样白血病（HL-60），肝癌（SMMC-7721）和肺癌（A549）的细胞毒活性。化合物37可以显着诱导SMMC-7721细胞的G2 / M期细胞周期停滞和凋亡。此外，化合物30在癌细胞（A549）和正常细胞（BEAS-2B）之间表现出一定程度的选择性细胞毒性。

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