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Nitrogen-containing heterocycles play a crucial role in medicinal chemistry and drug discovery, as several anticancer FDA-approved medicines are based on these compounds. Their structural and biological properties significantly impact their anticancer activity. Pyrazole and pyrimidine scaffolds show great anticancer potential. This review summarizes the synthesis and anticancer activity of several pyrazole and pyrimidine-based compounds, which exhibit great potential as cancer treatment candidates. The structural and biological characteristics of pyrazole and pyrimidine rings make them suitable scaffolds for designing novel anticancer agents. This review describes various synthetic routes for the preparation of pyrazole and pyrimidine derivatives, as well as their mechanisms of action in cancer therapy. These compounds exhibit potent cytotoxicity against breast, lung, and colon cancer cell lines. A detailed synthesis scheme shows how to incorporate pyrazole and pyrimidine scaffolds into medicinal compounds. Recent studies suggest that these derivatives exhibit substantial antitumor effects, supporting their development as targeted cancer therapies. Through the detailed description of synthesis, mechanisms of action, and anticancer activity, this review provides useful information on pyrazole and pyrimidine derivatives as potential future anticancer agents, highlighting their therapeutic potential in cancer treatment.
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