Nonactic acid, which is a macrocyclic nonactin subunit, contains four asymmetric centers and has the molecular formula of C10H18O3. Due to their various biological activities and challenging structural characteristics, nonactic acid and its derivatives have attracted much attention from scientists since 1955. These compounds possess significant antibacterial, insecticidal and acaricidal activities, as well as a promoting effect on plant growth. However, the studies in the anticancer activities of these compounds are limited. It is noticed that some derivatives of nonactic acid show significant cytotoxicity toward different human cancer cells, from which, a basic structure-activity relationship might be able to obtain. On the basis of these progresses, we believe that this review may provide new ideas for generating potent anticancer compounds bearing the same pharmacophores derived from those macrocyclic molecules.