Exploring novel classes of antitumor agents is an excellent approach to treat cancer diseases, which is responsible for major deaths worldwide. Pyrazolo[1,5-a]pyrimidine derivatives occupy a unique place in medicinal chemistry due to its various pharmacological activities. Besides, pyrazolo[1,5-a]pyrimidine derivatives are purine analogue of particular significance in medicinal chemistry due to their broad scope of remarkable antitumor activities. In this context, a new series of pyrazolo[1,5-a]pyrimidine derivatives were synthesized, characterized by their spectral data and screened for their antitumor activities.