Platinum complexes such as cisplatin and caboplatin are widely used in cancer chemotherapy. However, their clinical applications are substantially limited by unexpected toxic side effects. In this review, we discuss the current progress on the design and synthesis of estradiol-linked platinum complexes as the targeted antitumor drugs. Many of them display a high antitumor activity against the growth of breast cancer cell lines in vitro. The estradiol-linked platinum complexes could be used as target therapeutics for breast cancer.