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Background: Globally, cancer is the leading cause of death, which causes 10 million deaths yearly. Clinically, several drugs are used in treatment but due to drug resistance and multidrug resistance, there occurs a failure in the cancer treatment., Objectives: The present review article is a comprehensive review of pyrazole and pyrimidine hybrids as potential anticancer agents., Methods: The review comprises more than 60 research works done in this field. The efficiency of the reported pyrazolopyrimidine fused heterocyclic with their biological data and the influence of the structural aspects of the molecule have been discussed., Results: This review highlighted pyrazolo-pyrimidines as targeted anticancer agents with effect on multiple targets., Conclusion: The review will be helpful for the researchers involved in targeted drugs for cancer therapy for designing new scaffolds with pyrazolo-pyrimidine moieties., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)