: The quinolinic ring, present in several molecules, has a great diversity of biological activities. Therefore, this ring is in the structure composition of several candidates of drugs in preclinical and clinical studies, thus, it is necessary the grouping of these results to facilitate the design of new drugs. For this reason, some of the activities were selected for this review, such as: antimalarial, antimicrobial, anticancer, anti-inflammatory, antidiabetic, anti-rheumatic and antiviral. All publications of scientific articles chosen are dated between 2000 and 2020. In addition to presenting the structures of some natural and synthetic compounds with their activities, we list the clinical studies of phases III and IV of antimalarial drugs containing the quinoline nucleus and phase III clinical studies of hydroxychloroquine and chloroquine to assess their possible role in COVID-19. Finally, we show some of the mechanisms of action, as well as the side effects of some of the quinolinic derivatives.