Quinoline and its fused heterocyclic derivatives tested with diverse pharmacological activity functional groups constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. The present review provides an in depth view of work done so far on quinolines and its biological activities covering anticancer, antimycobacterial, antimicrobial, anticonvulsant, antiinflamatory and cardiovascular activities.