Cancer is one of the leading causes of death. Despite significant advancements in the discovery of medications for the treatment of cancer, these drugs are hindered by applicability and efficacy issues and frequently exhibit major side effects that can further impair patients 'quality of life. Therefore, the development of therapeutically sound anti-cancer medicines derived from natural products has gained prominence in the field of functional foods. Some of these compounds have shown efficacy in the prevention and treatment of cancer as well as low toxicity. Additionally, many recent studies have explored the recycling of agro-industrial waste to create bioactive chemicals. Citrus peels are produced in vast quantities in the food processing sector; due to their abundance of flavonoids, they may be inexpensive sources of protection against several cancers. Citrus is a common type of fruit that contains a variety of nutrients. In particular, the antioxidant chemicals found in citrus peel have been identified as potential cancer-fighting agents. Antioxidant substances such as flavonoids prevent the development of cancer by inhibiting the metastatic cascade, decreasing the mobility of cancer cells in the circulatory system, promoting apoptosis, and suppressing angiogenesis. To explore the most effective uses of citrus peel-derived antioxidants, this review presents background information, an overview of the role of citrus antioxidants in cancer therapy, and a discussion of the key underlying molecular mechanisms.