Cancer is the most-deadly disease having the most formidable afflictions in the world. Numerous anticancer drugs are available commercially, but the development of acquired drug resistance and the severe side effects of these clinically utilised anticancer drugs pose significant obstacles to the effective chemotherapy. Consequently, the rational design of novel medications with minimal adverse effects is advised. Due to their excellent pharmacological and pharmacokinetic characteristics, fluoroquinolone derivatives are of utmost interest to scientists. They display a number of positive traits, such as increased bioavailability, superior tissue penetration, and a relatively low prevalence of negative effects. The emphasis of the field of research is currently shifting towards these chemicals' anticancer properties because of their potential to intervene in mutagenesis and carcinogenesis. This study outlines current developments in the creation of new fluoroquinolones as prospective cytotoxic and anticancer medicines as well as their potential mechanisms of action for future research. Additionally, this review aims to concentrate on the numerous forthcoming characteristics of fluoroquinolones and offers a fresh perspective on their potential applications in the treatment of cancer.