Wheat (Triticum aestivum L.) is one of the most commonly cultivated and consumed cereals throughout the world. Though phytochemicals and antioxidants in the cereal grains have not been studied as in fruits and vegetables, given the role of wheat in our diet plate, it is a given of primary importance to understand the chemistry of our major food, wheat. The presence of diverse polyphenols and their action against leading cause of death, including heart diseases, cancer, obesity, and diabetes, widens the scope of wheat. Phytochemicals such as phenolic acids, alkylresorcinols, flavonoids, phytosterols, and carotenoids are present in whole wheat. The majority of phytochemicals are located in the wheat bran/germ fraction, and they are the leading contributors to the health promoting activities. However, the presence of anti-nutrients and binding of phenolic acids with protein may have adverse effect on health. This review mainly focuses on studies that have been carried out in the past decade to present, emphasizing the importance of whole wheat and whole wheat based products in preventing major diseases and disease conditions, potentials threats, current lacks, and future prospects.