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Low generation triazine-based dendrimers-synthesis, characterzation and in vitro biological activity

机译:低代三嗪基树枝状聚合物的合成,表征及体外生物活性

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摘要

In the present study, two low generation triazine-based dendrimers, G1.0(Cl)4 dendrimer and G1.5(OH)8 dendrimer, were synthesized and their cytotoxicity were tested by using the NIH 3T3 and the A2780 cell lines. In the synthesis process of the G1.0(Cl)4 dendrimer, cyanuric chloride (CAC) which has high reactivity chlorine atom was connected to the terminal of triethylene glycol (TEG) via nucleophilic substitution by controlling temperature. The prepared G1.0(Cl)4 dendrimer was purified by silica gel column chromatography. Then the four chlorine atoms in the G1.0(Cl)4 dendrimer were substituted by diethanolamine (DEA) to give dendrimer with the hydroxyl terminal group G1.5(OH)8. The starting materials, CAC, G1.0(Cl)4 dendrimer and G1.5(OH)8 dendrimer were analyzed by one-dimensional NMR, FTIR and MS techniques. The two dendrimers, G1.0(Cl)4 and G1.5(OH)8, showed perfect stability in the air environment at room temperature. However, G1.0(Cl)4 is not soluble in water while the G1.5(OH)8 dendrimer is a water soluble compound. Furthermore, cell biological evaluation at the studied concentrations showed that the CAC, as well as the prepared G1.0(Cl)4 and G1.5(OH)8 dendrimers, have no cytotoxicity towards the NIH 3T3 and A2780 cell lines.
机译:在本研究中,合成了两种低代三嗪基树枝状大分子G1.0(Cl)4树枝状大分子和G1.5(OH)8树枝状大分子,并使用NIH 3T3和A2780细胞系测试了它们的细胞毒性。在G1.0(Cl)4树枝状聚合物的合成过程中,通过控制温度,通过亲核取代将具有高反应性氯原子的氰尿酰氯(CAC)连接至三甘醇(TEG)的末端。制备的G1.0(Cl)4树枝状聚合物通过硅胶柱色谱法纯化。然后,将G1.0(Cl)4树枝状聚合物中的四个氯原子用二乙醇胺(DEA)取代,得到带有羟基端基G1.5(OH)8的树枝状聚合物。通过一维NMR,FTIR和MS技术分析了原料CAC,G1.0(Cl)4树枝状聚合物和G1.5(OH)8树枝状聚合物。两种树枝状聚合物G1.0(Cl)4和G1.5(OH)8在室温下在空气环境中显示出完美的稳定性。但是,G1.0(Cl)4不溶于水,而G1.5(OH)8树枝状聚合物是水溶性化合物。此外,在研究浓度下的细胞生物学评估表明,CAC以及制备的G1.0(Cl)4和G1.5(OH)8树状聚合物对NIH 3T3和A2780细胞系均无细胞毒性。

著录项

  • 作者

    Zhang Xupeng;

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  • 年度 2015
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  • 原文格式 PDF
  • 正文语种 eng
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