Cancer stands as the second most common cause of disease-related death in humans. Although numerous anticancer drugs are available, mostly they are expensive with serious side effects. Thus, the challenging task of finding an alternative cancer treatment measure has become more important than ever to both scientists and physicians. Since natural compounds are known for their various health benefits for centuries, several nutritional factors have brought considerable attention as modifiable risk factors in the prevention and treatment of cancer. Based on currently available research, the present chapter focuses on the chemo preventive and chemotherapeutic properties of different natural/dietary compounds such as fruits, vegetable, spices, nuts, legumes, cereals and grains highlighting their potential use against cancer treatment. The molecular mechanisms by which theses dietary compounds inhibit cancer development and induce cell death are also included to a certain extent.