Quercetin, a major representative of the flavonol subclass found abundantly in almost all edible vegetables and fruits, showed remarkable therapeutic properties and was beneficial in numerous degenerative diseases by preventing lipid peroxidation. Quercetin is beneficial in different diseases, such as atherosclerosis and chronic inflammation. This study aims to find out the anticancer activities of quercetin and to determine different mechanisms and pathways which are responsible for the anticancer effect. It also revealed the biopharmaceutical, toxicological characteristics, and clinical utilization of quercetin to evaluate its suitability for further investigations as a reliable anticancer drug. All of the relevant data concerning this compound with cancer was collected using different scientific search engines, including PubMed, Springer Link, Wiley Online, Web of Science, SciFinder, ScienceDirect, and Google Scholar. This review demonstrated that quercetin showed strong anticancer properties, including apoptosis, inhibition of cell proliferation, autophagy, cell cycle arrest, inhibition of angiogenesis, and inhibition of invasion and migration against various types of cancer. Findings also revealed that quercetin could significantly moderate and regulate different pathways, including PI3K/AKT‐mTORC1 pathway, JAK/STAT signaling system, MAPK signaling pathway, MMP signaling pathway, NF‐κB pathway, and p‐Camk2/p‐DRP1 pathway. However, this study found that quercetin showed poor oral bioavailability due to reduced absorption; this limitation is overcome by applying nanotechnology (nanoformulation of quercetin). Moreover, different investigations revealed that quercetin expressed no toxic effect in the investigated subjects. Based on the view of these findings, it is demonstrated that quercetin might be considered a reliable chemotherapeutic drug candidate in the treatment of different cancers. However, more clinical studies are suggested to establish the proper therapeutic efficacy, safety, and human dose.