Cancer, a disease characterized by high incidence, morbidity, and mortality rates, represents a significant challenge in global public health, requiring continuous efforts from the scientific community. A promising perspective in the battle against this disease emerges with food bioactives. When found in vegetables, these compounds are known as phytochemicals or phytonutrients, being secondary metabolites produced by plants as part of their self-defense. They exhibit physiologically active properties that go beyond basic nutrition, providing benefits to human health. Numerous food bioactives have already demonstrated to be useful in cancer prevention and therapy due to their antioxidant, anti-inflammatory, and chemopreventive properties. In vivo and in vitro studies suggest that these compounds can regulate the carcinogenesis process by targeting several molecules and signaling pathways. Some suggested mechanisms of action include inhibiting cancer cell growth, modulating the cell cycle, inducing apoptosis, reducing angiogenesis, and modulating redox imbalance that damages DNA. In addition to their preventive role, some bioactives have shown promise in combined therapy with conventional treatments or as alternative therapeutic approaches. In this chapter, we delve deeper into the prospecting of bioactives from plant matrices, with focus in phytochemicals, as well as their metabolic and genetic modulation effects related to anticancer therapeutic properties.