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Estrogen-dependent breast cancer (EDBC) is a kind of common malignant tumor in postmenopausal women with growing tendency in recent years. Aromatase (AR) is the key enzyme responsible for estrogen biosynthesis and has been considered as an important target for designing inhibitors as potent therapeutic agents for EDBC. AR inhibitors (AIs) are divided into steroidal and nonsteroidal compounds, and the latter shows high inhibitory potency against AR. This review summarizes recent advancement in nonsteroidal AIs.