New drugs introduced in the market each year, have privileged structures specifically
for anticancer targets, of which quinoline-based analogues also play an important role. This review
highlights quinoline and its derivatives, which have great potency against various cancer cells,
including prostate cancer, breast cancer, colon cancer, pancreas cancer, and many more. This review
describes the most preferred process-scale synthetic approaches of quinoline and its derivatives
having a specific pharmacophore for anticancer targets. It also describes the undergoing development
and recently approved drugs in tabular form. Quinoline moiety as a privileged structural
pharmacophore has the most effective activity against different cancer cell lines like prostate
cancer, breast cancer, stomach cancer, pancreas cancer, Colon cancer, CNS cancer, and renal cancer.
It can be used as a lead compound for further research on anticancer drug discovery.