Cancer is a very risky life-threatening disease having most formidable afflictions in the world. Several anticancer agents are commercially accessible, however, the emergence of acquired drug resistance along with extreme adverse effects of these clinically used anticancer medications are major barriers to the effective chemotherapy. Different studies have been established on the anticancer potential of several medically used antibacterial fluoroquinolones. Fluoroquinolone derivatives, like some anti‐ cancer drugs, such as doxorubicin, can achieve antitumor activity via poisoning of type II human DNA topoisomerases. Interestingly, structural features required for the anticancer activity of quinolones have been determined. Due to the limited data available on several of the agents, the criteria for inclusion of the study in the in vitro, pharmacokinetics and in vivo sections were not restrictive. The new fluoroquinolones offer excellent anticancer activity. All of the new fluoroquinolones have a longer serum half-life, and several are eliminated predominantly by nonrenal means. This review highlights the antitumor potential of fluoroquinolones in general and summarizes the chemical modifications carried out on fluoroquinolones to become anticancer agents. Moreover, this review gives a quick recap on metal ion chelates with fluoroquinolones and their substantial role in topoisomerase poisoning and potential antitumor improvement. Therefore, it should be highly interesting for researchers attempting to design and synthesize novel anticancer fluoroquinolone candidates.

Fluoroquinolones; quinolones, anticancer, mechanism of action