Abstract::PI3K is an important anticancer target as it controls cellular functions such as growth, transformation, proliferation,
motility and differentiation. Plasma cell cancer (multiple myeloma) occurs more than 10% among all haematological
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, gefitinib,
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.