Cancer is the world's devastating disease, and breast cancer is the most common reason for the death of women worldwide. Many synthetic drugs and medications are provided with their beneficial actions, but all of these have side effects and resistance problems. Natural remedies are coming forward to overcome the disadvantages of synthetic drugs. Among the natural categories, phytoestrogens having a structural similarity of mammalian oestradiol proves its benefit with various mechanisms not only in the treatment of breast cancer but even to prevent the occurrence of postmenopausal symptoms. Phytoestrogens are plant-derived compounds that were utilized in ancient medications and traditional knowledge for its sex hormone properties. Phytoestrogens exert pleiotropic effects on cellular signalling and show effects on estrogen-dependent diseases. However, because of activation/inhibition of steroid hormonal receptor ER-α or ER-β, these compounds induce or inhibit steroid hormonal (estrogen) action and, therefore, have the potential to disrupt hormone (estrogen) signalling pathway. In this review, we have discussed and summarize the effect of certain phytoestrogens and their possible mechanisms that can substantiate advantageous benefits for the treatment of post-menopausal symptoms as well as for breast cancer.