Abstract Cancer remains one of the most formidable pathological conditions, necessitating early diagnosis and the development of effective therapeutic strategies. Quinoxaline derivatives have emerged as promising candidates among nitrogen‐containing heterocyclic compounds due to their diverse pharmacological profile. This review critically examines the anticancer potential of quinoxaline scaffolds through their ability to modulate multiple oncogenic pathways simultaneously. Notably, these compounds demonstrate potent inhibitory effects against critical targets such as tubulin polymerization, c‐Met kinase, topoisomerase II, and EGFR kinase, while also inducing apoptosis, arresting cell cycle progression, and inhibiting FLT3, JAK2, VEGFR2, SIRT1, and PI3Kα signaling pathways. This review highlights recent advancements in the synthesis of quinoxaline derivatives, with a particular focus on nanocatalyst‐based approaches and the use of nano‐carriers. The integration of nanocatalyst‐based synthetic approaches represents a significant advancement over conventional methods, providing eco‐friendly, efficient, and high‐yield processes. Furthermore, structure–activity relationship analysis provides critical insights for rational drug design, revealing key molecular determinants that enhance potency and selectivity against specific cancer targets. By bridging nanotechnology with medicinal chemistry, this review demonstrates how quinoxaline derivatives can be strategically modified to overcome challenges in targeted cancer therapy, offering promising directions for developing next‐generation anticancer agents with improved efficacy and reduced toxicity profiles.
Sharma et al. (Fri,) studied this question.