Cancer is a global serious life threatening disease; it exerts massive impacts on diseased human body, and causes high rate of mortality in different parts of the world. It arises from irregular cell growth forming heterogenous tissues affecting normal ones' efficacies. Additionally, it can affect any body part and possess ability to migrate to another body organ, which is called metastasis. The real awful effect of cancer motivated many researchers to achieve synthesis of effective and safe anticancer drugs with the least possible side effects on normal body tissues. Among these trials heterocyclic derivatives gained vast interest, especially the imidazo- and pyrazo- pyrimidine ones. Many of these analogues exhibited good antitumor effects, even, some of them were approved by FDA as effective anticancer drugs. Through this review, we aimed to cover recent publications concerning synthesis of pyrimidine derivatives with either imidazole or pyrazole moieties and their effects as anticancer agents.