Carborane is a carbon-boron molecular cluster that can be viewed as a 3D analog of benzene. It features special physical and chemical properties, and thus has the potential to serve as a new type of pharmacophore for drug design and discovery. Based on the relative positions of two cage carbons, icosahedral closo-carboranes can be classified into three isomers, ortho-carborane (o-carborane, 1,2-C₂B₁₀H₁₂), meta-carborane (m-carborane, 1,7-C₂B₁₀H₁₂), and para-carborane (p-carborane, 1,12-C₂B₁₀H₁₂), and all of them can be deboronated to generate their nido- forms. Cage compound carborane and its derivatives have been demonstrated as useful chemical entities in antitumor medicinal chemistry. The applications of carboranes and their derivatives in the field of antitumor research mainly include boron neutron capture therapy (BNCT), as BNCT/photodynamic therapy dual sensitizers, and as anticancer ligands. This review summarizes the research progress on carboranes achieved up to October 2021, with particular emphasis on signaling transduction pathways, chemical structures, and mechanistic considerations of using carboranes.

碳硼烷是一种碳硼分子簇，可以视为苯的 3D 类似物。它具有特殊的物理和化学性质，因此有潜力作为药物设计和发现的新型药效团。根据两个笼碳的相对位置，二十面体近碳硼烷可分为三种异构体：邻碳硼烷（o-碳硼烷，1,2-C ₂ B ₁₀ H ₁₂）、间碳硼烷（m-碳硼烷，1 ,7-C ₂ B ₁₀ H ₁₂ )和对-碳硼烷( p-碳硼烷,1,12-C ₂ B ₁₀ H ₁₂ )，并且它们都可以脱硼以生成它们的nido-形式。笼状化合物碳硼烷及其衍生物已被证明是抗肿瘤药物化学中有用的化学实体。碳硼烷及其衍生物在抗肿瘤研究领域的应用主要包括硼中子俘获疗法（BNCT）、作为BNCT/光动力疗法双重增敏剂、作为抗癌配体。本综述总结了截至 2021 年 10 月关于碳硼烷的研究进展，特别强调了信号转导途径、化学结构以及使用碳硼烷的机制考虑。