Tubulin plays an important role in cell growth,morphological maintenance,signal transduction and mitotic process.Tubulin inhibitors are the popular antitumor drugs in recent years.Combretastatin A-4(CA-4) is one of the tubulin inhibitors,which is extracted and isolated from the Combretum caffrum in South African.It is one of the most active compounds with tubulin-inhibiting activity,but has many defects.Currently,researchers have designed other derivatives,focusing on how to improve the water solubility while keep the yield-configuration.In this article we reviewed the structure modification and the progress in CA-4 analogue design.