Abstract
The quinazolinone scaffold is widely present in natural compounds and serves as a core structural unit in various alkaloids. Its structural flexibility is a major advantage in anti‑tumor drug development. Characterized by a fused bicyclic system, this scaffold enables precise pharmacological modulation through targeted chemical modifications, allowing the regulation of multiple cell death pathways, including apoptosis, autophagy, ferroptosis, senescence, pyroptosis and necrosis. This review systematically describes the molecular mechanisms by which quinazolinone derivatives induce tumor cell death and critically evaluates their clinical translation potential. In addition, quinazolinone‑based agents approved by the Food and Drug Administration and those in preclinical development as targeted anti‑tumor therapies are summarized, providing new perspectives and methodological frameworks for advancing oncology drug discovery.