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Cereal products are the most important dietary source for energy intake and several bioactive compounds with high concentrations in the bran and the germ. Different cereal products provide a rich source of bioactive phytochemicals, namely, phenolic acids, carotenoids, tocopherols, alkylresorcinols, benzoxazines, phytosterols, and lignans. The bioactive substance alkylresorcinols (ARs) present in the whole cereal can inhibit enzyme activity, prevent bacterial or fungal infection, reduce cholesterol absorption, prevent cancer, and resist oxidation. In this paper, we discussed the biological activity of ARs in whole cereal products. Understanding the effects of processing on cereal phytochemicals will help us to develop improved processes for processing cereal foods with higher retention rates of bioactive compounds.