Microtubules (composed of α- and β-tubulin heterodimers) ubiquitous cellular polymers are important components of the cytoskeleton and play diverse roles within the cell, such as maintenance of cell structure, protein trafficking or chromosomal segregation during cell division. The polymers of tubulin play a pivotal role in mitosis and are regarded as an excellent target for chemotherapeutic agents to treat cancer. This review presents a brief overview of the synthesis and mechanism of action of new compounds targeting the dynamic of microtubule – tubulin polymerization/depolymerization. It is divided into the following parts: section I concerns targeting microtubules- tubulin-binding drugs derivatives of stilbene. In section II there are presented photoswitchable inhibitors of microtubule dynamics. Section III concerns using macrocyclic compounds as tubulin inhibitors. In this review, the authors focused primarily on reports produced inthe last five years and the latest strategies in this field.