Stilbenes are polyphenolic substances that are found in plants such as peanuts, grapes, and berries. Some of these compounds have demonstrated strong anticancer potential via multiple mechanisms. Pterostilbene and resveratrol have been shown to inhibit cancer cell proliferation, promote apoptosis, and inhibit the spread of cancer to other parts of the body. They can disrupt important molecular pathways, which ultimately results in the stoppage of the cell cycle, the activation of apoptosis, the prevention of angiogenesis, and the suppression of tumor invasion and metastasis. Stilbenes also possess powerful anti-inflammatory and antioxidant potential, which leads to their anticancer effects by lowering chronic inflammation and oxidative stress. Stilbenes are associated with multiple health benefits. On the other hand, their quick metabolism and low bioavailability make it difficult to use them in clinical settings successfully. The solubility, stability, and targeted distribution of these substances have been improved via the development of synthetic derivatives and nanoformulations by researchers. Stilbenes and their derivatives are valuable as innovative chemopreventive and therapeutic agents in the field of cancer due to their ability to target several targets simultaneously and their low toxicity.