Raj, AdityaKumar, AdarshSingh, Ankit KumarSingh, HarshwardhanThareja, SureshKumar, Pradeep2024-01-212024-08-132024-01-212024-08-132023-01-191871520610.2174/1871520623666230116163424http://10.2.3.109/handle/32116/3588PI3K is an important anticancer target as it controls cellular functions such as growth, transformation, pro-liferation, motility and differentiation. Plasma cell cancer (multiple myeloma) occurs more than 10% among all haema-tological malignancies and accounts for 2% of all cancer-related deaths each year, it is mainly regulated by PI3K/AKT signaling cascade. Quinazoline derivatives have been reported as promising PI3K inhibitors. Lapatinib, afatinib, ge-fitinib, erlotinib, idelalisib and copanlisib are quinazoline-based, FDA-approved PI3K inhibitors, while compounds like NVPBYL719, GDC-0032, AZD8186, AZD-6482, etc. are under different stages of clinical trials. In light of the above-mentioned facts, in the present study, we have reported different synthetic approaches, mechanisms of anticancer action, and structure-activity relationship analysis of reported quinazoline derivatives as PI3K inhibitors to help researchers working in the field in designing better and isoform-selective PI3K inhibitors. � 2023 Bentham Science Publishers.en-USCancermechanism of actionmTOR pathwaysPI3KquinazolineSARReviewhttps://www.eurekaselect.com/212789/article