Imidazo[1,2-a]pyridine has been shown to be an important biologically active moiety. This
review is a compilation of the scattered output of results of the anticancer activities of the imidazo[1,2-a]pyridine system since 2001, which have been classified as inhibition of CDK, VEGFR,
PI3K, EGFR, RGGT etc. along with inhibition against different tumor cell lines. Various imidazo[1,2-a]pyridine based analogues have been used as lead molecules and are now under human
clinical trials. This review will help the wider scientific community in the area of drug discovery of
imidazo[1,2-a]pyridines as novel anticancer agents.