Due to its powerful anticancer characteristics, the heterocyclic quinazoline has attracted a lot of interest in cancer research. Several cancer types, including lung, breast, colon, ovarian, and prostate cancers, have shown promise in response to quinazoline compounds' potential inhibitory properties. Protein tyrosine kinases (PTKs) are one of the main mechanisms through which quinazoline exerts its anticancer effects. Quinazoline drugs can interfere with the signaling pathways that support tumor growth and survival by specifically targeting PTKs. Quinazoline derivatives also exhibit antiangiogenic properties by blocking the vascular endothelial growth factor (VEGF) pathway, which prevents the creation of new blood vessels needed to feed the tumor. Additionally, chemicals derived from quinazolines have the ability to cause cancer cells to undergo apoptosis, or the halt of the cell cycle. Furthermore, quinazolines can accelerate the death of cancer cells while sparing normal, healthy cells through altering the regulation of the cell cycle and pro-apoptotic signaling pathways. Due to their favorable pharmacokinetic profile and low toxicity, they are also promising candidates for further investigation as anticancer agents. More research is required to enhance their efficacy, selectivity, and safety characteristics. Overall, quinazoline and its derivatives have been considered as attractive candidates for further development of novel therapeutic strategies in the field of cancer therapy.