Microtubule plays an important role in the maintenance of cell shape and the process of signal transduction and mitosis.The drugs targeting microtubules induce apoptosis by blocking mitosis.Due to the extreme importance of microtubule in the process of mitosis,tubulin becomes one of the most important targets for development of new anticancer drugs.Colchicine binding site inhibitors (CSIs) is one of the major classes of tubulin polymerization inhibitors.Many CSIs have been discovered,designed or synthesized as anticancer agents in the past several years and great progress has been made.α-Methylene-γ-butyrolactone are important classes of natural products or synthetic bioactive molecules.