Plant bioactive compounds, spanning alkaloids, flavonoids, terpenoids, and polyphenols, hold significant promise as potent and safer anticancer agents. This review explores the diverse range of plant-derived compounds, including alkaloids, flavonoids, terpenoids, and polyphenols, investigating their mechanisms of action, preclinical and clinical evidence, and potential integration into cancer treatment regimens. Alkaloids like vincristine and vinblastine disrupt microtubule formation, inducing mitotic arrest and apoptosis. Flavonoids such as quercetin and epigallocatechin gallate exhibit antioxidant properties and modulate crucial signalling pathways in cancer cells. Terpenoids, exemplified by Texans and isoprenoids, target microtubules are signalling proteins for focused anticancer strategies. Polyphenols like resveratrol contribute to cancer prevention via antioxidant and anti-inflammatory mechanisms. Preclinical evidence underscores their efficacy, with more clinical trials completed for resveratrol than quercetin. Understanding their mechanisms, particularly of compounds like resveratrol and quercetin, sheds light on their specific targets within cancer cells. Exploring plant bioactive compounds presents a promising avenue for innovative and less toxic anticancer therapeutics, aligning with the global imperative to enhance cancer care.