Globally cancer is one of the leading causes of mortality. Although, rapid progression and advancement in treatment have been made to combat this life-threatening disease. Conventional therapies like chemotherapy and radiation therapy have several adverse side effects on healthy cells, therefore, a novel alternative and effective treatment regime is required to treat cancer. Currently, the benefits of using medicinal plant-derived products over synthetic medicine have significantly increased in the field of healthcare. Several medicinal plants and their bioactive compounds have shown to possess potent anti-cancer properties in vitro and in vivo. Additionally, they are less toxic, very effective and, safe when administered in cancer patients. Some of the well-established anti-tumor compounds include vinblastine, curcumin, vincristine, podophyllotoxin, taxol, orientin, camptothecin vinflunine ditartrate, anhydrovinblastine, poliglumex, combretastatins, and triptolide. Many of them are in clinical trial, only a few have been clinically approved. This chapter