Butterfly-shaped structure, as a novel scaffold with an attractive and certain shape, has been widely used in new drug discovery. Tubulin, composing of α- and β-tubulin heterodimers, plays a key role in mitosis and cell division which are regarded as an excellent target for cancer therapy. Currently, a series of butterfly shape diaryl heterocyclic compounds have been reported with strong potential against the tubulin-colchicine binding site. It is with one ring buried in the β subunit, another ring interacts with the α subunit and the main body is located in the flat pocket. Here, we firstly introduce the concept of butterfly structure for the tubulin inhibitors, focusing on the latest advancements in a variety of molecules bearing butterfly structure, and then highlight the challenges and future direction of butterfly structure- based tubulin-colchicine binding site inhibitors.

蝴蝶形结构作为具有吸引力和确定形状的新型支架，已被广泛用于新药开发中。微管蛋白由α-微管蛋白和β-微管蛋白异二聚体组成，在有丝分裂和细胞分裂中起着关键作用，被认为是癌症治疗的极佳靶标。目前，已经报道了一系列蝴蝶形的二芳基杂环化合物具有针对微管蛋白-秋水仙碱结合位点的强大潜力。它的一个环埋在β亚基中，另一个环与α亚基相互作用，主体位于扁平袋中。在这里，我们首先介绍微管蛋白抑制剂的蝶形结构概念，重点介绍各种带有蝶形结构的分子的最新进展，