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Background: This paper reviews the research progress of pyrazoloquinazolines which widely used in the field of medicine and pesticide in recent years. Five types of pyrazoloquinazolines are introduced: pyrazolo [4,3-h]quinazolines, pyrazolo[1,5-c]quinazolines, pyrazolo[4,3-f]quinazolines, pyrazolo[1,5-a] quinazolines , pyrazolo[1,5-b]quinazolines, and their new progress in the synthesis methods and treatment of diseases. Methodology: The derivatives of pyrazoloquinazolines exhibit a wide range of pharmacological properties such as antibacterial, anticancer, antioxidants, anti-inflammatory, anti-diabetic, antiviral activities. Consequently, their syntheses have attracted significant interest. Various methodologies have been developed for the synthesis and functionalization of these class of compounds. Conclusion: In the present article, the relevant and recent advances in the field will be briefly covered.