Introduction: Cancer remains a leading cause of death worldwide with traditional treatments like chemotherapy, and radiotherapy becoming less effective due to multidrug resistance (MDR). This highlights the necessity for novel chemotherapeutics like chalcone-based compounds, which demonstrate broad anti-cancer properties and target multiple pathways. These compounds hold promise for improving cancer treatment outcomes compared to existing therapies.
Areas covered: This review provides a comprehensive synopsis of the recent literature (2018-2024) for anti-proliferative/anti-cancer activity of chalcones. It includes the identification of potential targets, their mechanisms of action, and possible modes of binding. Additionally, chalcone derivatives in preclinical trials are also discussed.
Expert opinion: Chalcones mark a significant stride in anticancer therapies due to their multifaceted approach in targeting various cellular pathways. Their ability to simultaneously target multiple pathways enables them to overcome drug resistance as compared to traditional therapies. With well-defined mechanisms of action, these compounds can serve as lead molecules for designing new, more promising treatments. Continued progress in synthesis and structural optimization, along with promising results from preclinical trials, offers hope for the development of more potent molecules, heralding a new era in cancer therapeutics.
Keywords: Angiogenesis; chalcones; drug targets; kinases; microtubulin; synthesis; topoisomerases.