Caminade Anne-Marie, Milewski Max, Hey-Hawkins Evamarie
Laboratoire de Chimie de Coordination (LCC-CNRS) 205 Route de Narbonne, CEDEX 4, 31077 Toulouse, France.
LCC-CNRS, Université de Toulouse, CNRS, 31077 Toulouse, France.
Pharmaceutics. 2023 Aug 10;15(8):2117. doi: 10.3390/pharmaceutics15082117.
The presence of a large number of boron atoms in boron clusters make them attractive tools for the treatment of cancer using boron neutron capture therapy (BNCT). Since the quantity of boron atoms present in the target cell directly affects the effectiveness of BNCT, the idea of gathering a high number of boron atoms in a single entity has emerged many years ago. In this perspective, using hyper-branched macromolecules such as dendrimers appears as an interesting solution. In this review, we will first present the synthesis of diverse dendritic entities (dendrimers, dendrons, and Janus dendrimers) that incorporate boron clusters, in particular carboranes, anywhere in their structure. Four parts of this review present the synthesis of dendrimers having boron clusters on the surface, or inside their structure, of dendrons and of Janus dendrimers, bearing boron clusters. Practically all these boronated dendritic structures were synthesized with the objective to study their biological properties, but in fact only a few of them have been tested against cancerous cells, and even a smaller number was tested in BNCT experiments. The biological experiments are discussed in the fifth part of this review. A good efficiency is generally observed with the boronated dendrimers, even in animal models, with an increase in their mean survival time (MST).
硼簇中大量硼原子的存在使其成为使用硼中子俘获疗法(BNCT)治疗癌症的有吸引力的工具。由于靶细胞中硼原子的数量直接影响BNCT的有效性,多年前就出现了在单个实体中聚集大量硼原子的想法。从这个角度来看,使用超支化大分子如树枝状大分子似乎是一个有趣的解决方案。在这篇综述中,我们将首先介绍各种包含硼簇(特别是碳硼烷)的树枝状实体(树枝状大分子、树枝状单体和Janus树枝状大分子)的合成,这些硼簇位于其结构的任何位置。本综述的四个部分分别介绍了表面带有硼簇、结构内部带有硼簇的树枝状大分子、带有硼簇的树枝状单体以及Janus树枝状大分子的合成。实际上,所有这些含硼树枝状结构的合成目的都是研究其生物学性质,但事实上,其中只有少数针对癌细胞进行了测试,在BNCT实验中测试的数量更少。生物学实验将在本综述的第五部分进行讨论。即使在动物模型中,含硼树枝状大分子通常也表现出良好的效果,其平均生存时间(MST)有所增加。