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Cancer is a group of diseases involving abnormal cell growth with the potential to spread to other parts of the body, is one of the most formidable afflictions in the world. However, 100% effective cancer treatment is not available. The design of cancer chemotherapy has become increasingly difficult. Currently, cancer therapy interfering with a single biological molecule or pathway has been successfully utilized. Chemotherapy can kill cancer cells that have spread to parts of the body. Therefore, agents like tubulin inhibitor are discovered to treat cancer. Tubulin inhibitors perform by interfering with the dynamics of the microtubule. As a result, there is increasing interest in the discovery of agents that concomitantly address more than one biological target for cancer treatment. Drugs that affect the tubulin-microtubule equilibrium are effective anticancer drugs. This book describes the molecular target, methods used in screening, the structures of compounds known to interactwith tubulin, the ability of these agents to destroy tumour vasculature and clinical use of these agents as exciting new molecular target in the design of anticancer drugs.