We designed and synthesized several families of novel amphiphilic fluorescent phosphorus dendron-based micelles showing relevant antiproliferative activities for use in the field of theranostic nanomedicine. Based on straightforward synthesis pathways, 12 amphiphilic phosphorus dendrons bearing 10 protonated cyclic amino groups (generation one), or 20 protonated amino groups (generation two), and 1 hydrophobic chain carrying 1 fluorophore moiety were created. The amphiphilic dendron micelles had the capacity to aggregate in solution using hydrophilic/hydrophobic interactions, which promoted the formation of polymeric micelles. These dendron-based micelles showed moderate to high antiproliferative activities against a panel of tumor cell lines. This paper presents for the first time the synthesis and our first investigations of new phosphorus dendron-based micelles for cancer therapy applications.

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作为抗增殖剂的两亲荧光磷树突基胶束的简便合成：初步研究

我们设计并合成了几个家族的新型两亲性荧光磷树枝状胶束，显示出相关的抗增殖活性，用于治疗纳米医学领域。基于直接的合成途径，产生了 12 个带有 10 个质子化环状氨基（第一代）或 20 个质子化氨基（第二代）和 1 个带有 1 个荧光团部分的疏水链的两亲性磷树突。两亲树枝状胶束具有利用亲水/疏水相互作用在溶液中聚集的能力，这促进了聚合物胶束的形成。这些基于树突的胶束对一组肿瘤细胞系显示出中等至高度的抗增殖活性。