Cancer is a disease in which some of the body's cells grow uncontrollably and spread to other parts of the body. Cancer treatment usually involves the use of single or combined strategies including surgery, radiotherapy and chemotherapy. Chemotherapy is most often used to treat cancer, since cancer cells grow and multiply much more quickly than most cells in the body. The dynamic equilibrium of tubulin-microtubule is an essential aspect of cell survival and tubulin is a significant target for cancer drug development. Tubulin exists in the α-β dimer form which polymerizes to form microtubule and further depolymerizes back to tubulin dimer. The microtubule plays an essential role in mitosis and cell multiplication. Disruption of microtubules can induce cell cycle arrest in G2-M phase and formation of abnormal mitotic spindles. A number of naturally occurring compounds such as combretastatin, colchicines, paclitaxel, epothilones and vinblastine affect cancer cells by changing dynamics of tubulin such as polymerization and depolymerization. In this review, we briefly introduce an overview of tubulin polymerization inhibitors.