Human diet comprises of polyphenolic compounds called the flavonoids which are universally present as constituents of food plants. The flavonoid derivatives found in many of our spices and plants have applications for prevention of diseases and as therapeutic agents in traditional medicines mainly in Asia. The flavonoid composition is most likely the key for the potential health benefits. The lower risks of colon, prostate and breast cancers in Asian population could be related to their vegetable and fruit rich diets containing many flavonoid derivatives. The question is whether these flavonoids mediate the protective effects of diets rich in these foodstuffs by acting as natural chemopreventive and anticancer agents. The current study summarizes the most recent advances providing new insights into the factors, regulation and molecular mechanisms underlying the promising anticarcinogenic activity of dietary flavonoids, their potential interactions with proteins and other dietary components.