Synthetic and SAR Progress of Pyrazole Scaffolds as Anti-Colorectal Cancer Agents: Insights from 2010-2025

Abstract:

Colorectal cancer (CRC) continues to pose a pressing challenge to global health, with rising incidence rates and treatment outcomes frequently impeded by drug resistance, systemic toxicity, and limited selectivity in current chemotherapy regimens. In this context, heterocyclic compounds, particularly pyrazole derivatives, have emerged as promising candidates in the quest for more effective anticancer agents. This review explores advancements in the design, synthetic methodologies, and development of structurally diverse pyrazole-based molecules for CRC therapy, highlighting their biological activity, mechanisms of action, and the critical role of structure-activity relationship (SAR) studies in optimizing therapeutic performance. The exponential growth of academic literature suggests that strategic modifications to the core pyrazole structure can significantly enhance both potency and selectivity against key CRC cell lines, such as HCT116, HT29, and SW620. This review aims to collate literature work reported by researchers (from 2010 to 2025) to provide an overview of the potential of pyrazole-based derivatives, especially against CRC. Unlike broader oncology reviews, this work focuses exclusively on the role of pyrazole in colorectal cancer (CRC). By systematically sourcing literature from verified databases, including PubMed and Google Scholar, we comprehensively compile and elaborate on SAR reported between 2010 and 2025, providing a targeted resource for CRC drug discovery.