一些苄基硫代氨基脲衍生物的合成及其对U87、MCF-7、A549、3T3和HUVEC细胞的细胞毒性评价

IF 1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY
Touba Eslaminejad, Yaghoub Pourshojaei, M. Naghizadeh, Hoda Eslami, Mohammad Daneshpajouh, A. Hassanzadeh
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引用次数: 1

摘要

铁稳态在肿瘤中被改变以响应铁依赖蛋白表达的扰动。因此,铁螯合剂使癌细胞更容易受到缺铁的影响。具有巯基氨基脲支架和金属络合物形成能力的化合物具有潜在的抗癌作用。设计并成功合成了一系列硫代氨基脲衍生物,并采用WST-1试剂比色法对其在肿瘤和实验室正常模型系统上的细胞毒性进行了检测。根据细胞毒性结果,一些化合物对癌变细胞系和健康细胞系均表现出高毒性作用。对U87和A549细胞株的毒性试验结果表明,在浓度高于10 ppm时,所有化合物的存活率均低于50%。MCF-7细胞系表现出大致相同的行为,存活率低于60%。与HUVEC细胞株相比,3T3对合成化合物表现出完全不同的行为,存活率超过50%。同时测定了选择性指数,根据研究结果可以得出,合成的化合物对3T3细胞株的细胞毒性谱有显著差异,表明这些化合物具有良好的抗癌作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of some benzylidene thiosemicarbazide derivatives and evaluation of their cytotoxicity on U87, MCF-7, A549, 3T3 and HUVEC cell lines
Iron homeostasis is altered in tumours in response to a perturbation in the expression of iron-dependent proteins. Therefore, iron chelators make cancerous cells more vulnerable to iron deficiency. Compounds having thiosemicarbazide scaffold with the ability to metal complex formation have the potential to act as anticancer. A series of thiosemicarbazide derivatives were designed, synthesized successfully and their cytotoxicity was then tested on some cancerous as well as laboratory normal model systems by using colorimetric assay based on WST-1 reagent. According to the cytotoxicity results, some compounds showed high toxicity effect on both the cancerous and healthy cell lines. The results of toxicity assays on U87 and A549 cell lines showed the survivability less than 50% at all concentrations higher than 10 ppm for all the synthesized compounds. The MCF-7 cell line approximately exhibited the same behaviour and had survivability less than 60%. The 3T3 in compared with HUVEC cell line showed a completely different behaviour against the synthesized compounds and had survivability more than 50%. The selectivity index was also measured and based on the study results this could be concluded that the cytotoxicity profile of the synthesized compounds on 3T3 cell line shows a significant difference, indicating a good anticancer effect for these compounds.
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来源期刊
CiteScore
1.80
自引率
0.00%
发文量
76
审稿时长
1 months
期刊介绍: The Journal of the Serbian Chemical Society -JSCS (formerly Glasnik Hemijskog društva Beograd) publishes articles original papers that have not been published previously, from the fields of fundamental and applied chemistry: Theoretical Chemistry, Organic Chemistry, Biochemistry and Biotechnology, Food Chemistry, Technology and Engineering, Inorganic Chemistry, Polymers, Analytical Chemistry, Physical Chemistry, Spectroscopy, Electrochemistry, Thermodynamics, Chemical Engineering, Textile Engineering, Materials, Ceramics, Metallurgy, Geochemistry, Environmental Chemistry, History of and Education in Chemistry.
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