Aromatase, a crucial enzyme assigned for transforming androgen into estrogen, has a vital function in the advancement of drug-resistant breast cancers that respond to endocrine treatments. Aromatase (CYP19A1) is a monooxygenase from the cytochrome P450 family that is involved in the conversion of androgens to estrogens. Breast cancer cells express aromatase activity, indicating that the tumor cells may be able to produce local estrogen. By inhibiting aromatase, serum estrogen levels decrease, which, in turn, hinders estrogen-driven cancer cell growth in hormone receptor-positive breast cancer cases. In this sense, the introduction of novel aromatase inhibitors could be a significant step forward in the fight against cancer. This is especially true in hormone-dependent cancers. Many compounds have been introduced as aromatase inhibitors, classified as steroidal or nonsteroidal. However, it should be noted that these drugs have encountered resistance in numerous cases, particularly in recent years. Thus, the search for new aromatase inhibitor drugs has always been critical. Newly, there seems to be a surge of enthusiasm in the discovery and production of molecules with dual inhibitory effects, which can inhibit two or more enzymes simultaneously. This method enables a significant reduction in potential drug resistance. The design of these compounds has an opportunity to significantly boost the efficacy of anti-cancer treatments by causing synergistic effects. This article offers a review of newly developed aromatase inhibitors with potential anticancer effects.

Keywords: COX-2; Dual-acting; anticancer; aromatase; aromatase inhibitors.; aromatase/COX-2.

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