Functional foods are the focus of attraction for well-being. The healthy living of Asians may be attributed to a diet enriched with soy isoflavones viz. genistein and daidzein which fills the gap of proteinaceous diet in vegetarians. Several factors, such as administration, dosage, metabolism, ingestion of other pharmacological substances, type of estrogen receptors, and presence or absence of endogenous estrogen, affect the activities and bioavailability of isoflavones. The mode of therapeutic action could be either through the stimulation of estrogen receptors or by the non-involvement of estrogen receptors. Soy, due to its isoflavones content, serves as a balanced and remedial substitute in combating various lifestyle disorders, like cancer prevention, by interruption of the breakdown of extracellular matrix that surrounds growing vessels and tumors, lowering of lipid and blood insulin levels by regulating lipid and glucose metabolism, alleviation of menopausal symptoms, and osteoprotective effects by modulating estrogen receptors, thus acting as a safer switch to hormone replacement therapy, anti-hypertensive effect which may also contribute to cardioprotective, anti-oxidative effect, regulation of cognitive functions, and many others. Therefore, it could be regarded as a valuable therapeutics. However, since soy isoflavones also act as endocrine disruptors, they also possess some negative effects. Concerns have been raised in relation to thyroid function abnormality. In view of the previously mentioned facts an attempt has been made to review the literature available on both beneficial as well as deleterious role of isoflavones, soy derived bioactive compounds.