Cancer, which has been cursed for human beings for long time is considered as one of the
leading causes of morbidity and mortality across the world. In spite of different types of treatments
available, chemotherapy is still deemed as a favored treatment for the cancer. Unfortunately, many currently
accessible anticancer agents have developed multidrug resistance along with fatal adverse effects.
Therefore, intensive efforts have been made to seek for new active drugs with improved anticancer efficacy
and reduced adverse effects. In recent years, the emergence of heterocyclic ring-containing anticancer
agents has gained a great deal of attention among medicinal chemists. 1,3- oxazole is a versatile
heterocyclic compound, and its derivatives possess broad-spectrum pharmacological properties, including
anticancer activity against both drug-susceptible, drug-resistant and even multidrug-resistant cancer
cell lines through multiple mechanisms. Thus, the 1,3-oxazole moiety is a useful template for the development
of novel anticancer agents. This review will provide a comprehensive overview of the recent
advances on 1,3-oxazole derivatives with potential therapeutic applications as anticancer agents, focus
on the chemical structures, anticancer activity, and mechanisms of action.