<p>Cancer continues to be a primary cause of death globally, underscoring the urgent need for the ongoing development of innovative and effective therapeutic agents. Among various heterocyclic frameworks, pyrazole has emerged as a significant pharmacophore in medicinal chemistry due to its structural adaptability, advantageous pharmacokinetic characteristics, and a wide range of biological activities. This review provides a thorough overview of recent progress in the design, biological assessment, mechanistic understanding, and structure–activity relationships (SAR) of pyrazole-based derivatives with anticancer potential, while also briefly discussing notable synthetic methods documented in the literature. The compounds reviewed demonstrate encouraging activity against a variety of cancers, including breast, lung, colon, pancreatic, and hematological malignancies, through several mechanisms such as kinase inhibition, induction of apoptosis, cell-cycle arrest, epigenetic modulation, inhibition of angiogenesis, and suppression of metastasis. SAR analysis indicates that substitution patterns, heterocyclic fusion, optimization of linkers, and hybridization of pharmacophores are crucial in enhancing potency, selectivity, and target specificity. Numerous pyrazole derivatives show nanomolar activity and selective cytotoxicity towards cancer cells, emphasizing their potential as lead compounds for anticancer drug development. However, the majority of these candidates remain in the preclinical phase, highlighting the necessity for further pharmacokinetic, toxicological, and clinical studies. In summary, pyrazole-based scaffolds offer a promising foundation for the creation of next-generation anticancer therapeutics and require ongoing interdisciplinary research to promote their clinical application.</p> Graphical abstract <p></p>