So far, studies have demonstrated that salicylic acid derivatives including aspirin, sodium salicylate and copper salicylate are effective in inhibiting the growth of breast cancer. Among them, aspirin is the mostly studied salicylic acid derivatives, and its molecular mechanism of anticancer mainly include suppressing COX enzyme activity and regulating expressions of many important proteins such as NF-κB. To further develop those derivatives as therapeutic drugs for breast cancer, here we mainly reviewed the researches of salicylic acid derivatives in inhibiting breast cancer proliferation and its mechanism of action.