Introduction: For thousands of years, plants have been used as the main source of drug worldwide. Recently, it has been found out that the plant Artemisia annua and especially its derivatives such as artemether have anticancer properties. Methods: In this study, the anticancer effect of artemether on MCF-7 breast cancer cell line was examined. MTT assay was used to assess the viability of cancer cells. Results: The data showed that artemether (100-300 nM) resulted in MCF-7 growth inhibition. Artemether plus vincristine or doxorubicin compared to each drug alone showed significant cytotoxic effects. Over 50 percent of cells were killed in combination of non-effective doses of artemether and doxorubicin (50 and 160 nM, respectively). Conclusion: Taken together, the combined therapy of artemether and anticancer drugs would be a promising strategy for breast cancer but the effectiveness of such combination therapy needs to be verified by experimental and clinical investigations.