芳香酶抑制被认为是治疗 ER 阳性 (ER) 乳腺癌的合法方法，因为它占乳腺癌病例的 70% 以上。芳香酶抑制剂疗法已被证明在缩小肿瘤大小、提高生存率和降低癌症复发机会方面非常有效。本综述探讨了芳香酶在雌激素生物合成中的病理生理学和作用。还讨论了雌激素生物合成、各种雄激素及其在人体内的功能。已经简要讨论了芳香酶活性位点、其作用方式和 AI 的突出方面，以及它们与目前 FDA 批准的抑制剂的预期相互作用。它详细介绍了不同报道的人工智能是如何设计的、它们的 SAR 研究、计算机分析和生物学评估。还讨论了来自多个来源的各种人工智能，例如合成和半合成。版权所有 © 2024 Elsevier Inc. 保留所有权利。

Aromatase inhibition is considered a legitimate approach for the treatment of ER-positive (ER+) breast cancer as it accounts for more than 70% of breast cancer cases. Aromatase inhibitor therapy has been demonstrated to be highly effective in decreasing tumour size, increasing survival rates, and lowering the chance of cancer recurrence. The present review deliberates the pathophysiology and the role of aromatase in estrogen biosynthesis. Estrogen biosynthesis, various androgens, and their function in the human body have also been discussed. The salient aspects of the aromatase active site, its mode of action, and AIs, along with their intended interactions with presently FDA-approved inhibitors, have been briefly discussed. It has been detailed how different reported AIs were designed, their SAR investigations, in silico analysis, and biological evaluations. Various AIs from multiple origins, such as synthetic and semi-synthetic, have also been discussed.Copyright © 2024 Elsevier Inc. All rights reserved.