Coumarin derivatives have attracted substantial scientific interest due to their broad therapeutic potential in the field of oncology research due to their anticancer potential. Both naturally occurring and synthetically modified coumarins possess diverse pharmacological activities, and evidence highlights their strong anticancer properties. Studies emphasize the importance of understanding molecular mechanisms and structural interactions that govern the biological actions of coumarin hybrids, as these insights are crucial for optimizing their therapeutic efficacy in term of treatment. Coumarin-based hybrid compounds demonstrate the ability to modulate multiple cellular signalling pathways critical for cancer progression, including those regulating apoptosis, angiogenesis, oxidative stress, and uncontrolled cell division. Mechanistic studies show that many coumarin hybrids effectively induce apoptosis through mitochondrial disruption, caspase activation, and modulation of pro and anti-apoptotic proteins. Additionally, several derivatives exhibit potent anti-angiogenic activity by inhibiting VEGF-mediated signaling, thereby limiting tumor vascularization and growth. Their capacity to interfere with cell cycle regulators, such as cyclins and CDKs, further contributes to their antiproliferative effects. The multitargeted nature of these molecular interactions highlights the therapeutic versatility of coumarin hybrids. Overall, the emerging preclinical evidence positions coumarin derivatives as promising lead compounds for anticancer drug development, warranting further investigation through advanced pharmacological, structural, and clinical studies.
