首页> 外文期刊>Chemistry: A European journal >Tailored Control and Optimisation of the Number of Phosphonic Acid Termini on Phosphorus-Containing Dendrimers for the Ex-Vivo ACHTUNGTRENUNGActivation of Human Monocytes
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Tailored Control and Optimisation of the Number of Phosphonic Acid Termini on Phosphorus-Containing Dendrimers for the Ex-Vivo ACHTUNGTRENUNGActivation of Human Monocytes

机译:人眼单核细胞体外活化的含磷树枝状聚合物上的末端酸磷酸酯的量身定制控制和优化

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摘要

The syntheses of a series of phosphonic acid-capped dendrimers is described. This collection is based on a unique set of dendritic structural parameterscyclo(triphosphazene) core, benzylhydrazone branches and phosphonic acid surfaceand was designed to study the influence of phosphonate (phosphonic acid) surface loading towards the activation of human monocytes ex vivo. Starting from the versatile hexachloro-cyclo(triphosphazene) N3P3Cl6, six first-generation dendrimers were obtained, bearing one to six full branches, that lead to 4, 8, 12, 16, 20 and 24 phosphonate termini, respectively. The surface loading was also explored at the limit of dense packing by means of a first-generation dendrimer having a cyclo(tetraphosphazene) core and bearing 32termini, and with a first-generation dendrimer based on a AB2/CD5 growing pattern and bearing 60 termini. Human monocyte activation by these dendrimers confirms the requirement of the whole dendritic structure for bioactivity and identifies the dendrimer bearing four branches, thus 16 phosphonate termini, as the most bioactive.
机译:描述了一系列膦酸封端的树枝状大分子的合成。该集合基于一组独特的树状结构参数环(三磷腈)核心,苄hydr支链和膦酸表面,并且旨在研究膦酸酯(膦酸)表面负载对离体人类单核细胞活化的影响。从通用的六氯环(三磷腈)N3P3Cl6开始,获得了六个第一代树枝状大分子,带有一个至六个完整分支,分别导致4、8、12、16、20和24个膦酸酯末端。还通过具有环(四磷腈)核和32末端的第一代树枝状聚合物,以及基于AB2 / CD5生长模式和60末端的第一代树枝状聚合物,在致密堆积的极限处探索了表面载荷。 。这些树状聚合物对人单核细胞的激活证实了整个树状结构具有生物活性的要求,并确定了具有四个分支的树状聚合物,即16个膦酸酯末端是最具生物活性的。

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