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.
Keywords: Butterfly structure, Cancer, Diaryl heterocyclic, Tubulin-colchicine Binding site, Inhibitors, β-lactam.
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