Chemistry of heterocyclic organic compounds is as logical as that of aliphatic/aromatic compounds and of great interests both from the theoretical as well as practical synthetic view to design novel compounds that becomes one of the most important areas of research today. Electron-flux of six member/annulated N heterocycles plays vital roles to exhibit diverse potent biological activities from pharmaceuticals to industrial materials. The Pyrimidine and fused pyrimidine annulated rings in the chemistry of biological systems has attracted much attention due to availability in the substructures of therapeutic imperative natural products. As a result of their prominent and remarkable pharmacological activity, pyrimidine derivative’s intensive research has been made especially focused on its anticancer activity. The present review gives brief information about anticancer activity of assorted six member/annulated pyrimidine derivatives.