A large number of world women populations are suffering from breast cancer. It is increasing day by day that is quite alarming. The major reason behind breast tumors is upregulation of estrogen which is dependent on aromatase. Aromatase inhibitors (AIs) have opened up a new era to combat the battle against estrogen-mediated breast cancer. Despite several advantages, various adverse effects have limited the use of AIs. Therefore, it is still a demanding and challenging job to design selective AIs with fewer adverse effects. In this article, comparative quantitative structure-activity relationship (QSAR) study of steroidal aromatase inhibitors (SAIs) have been discussed in details to get an insight into the structural and physicochemical properties of SAIs controlling the aromatase inhibitory activity. This study reflects that SAIs should possess smaller shape and size with less bulky substituents having lesser polarity and less steric effect along with greater hydrophobicity for the higher aromatase inhibitory activity. This study will obviously shed light into the newer idea for the medicinal chemists to design and discover novel, effective and less toxic SAIs to combat the life-threatening breast cancer as well as to initiate a modern era in breast cancer drug discovery.

世界上许多妇女都患有乳腺癌。每天都在增加，这令人震惊。乳腺肿瘤背后的主要原因是依赖芳香化酶的雌激素上调。芳香酶抑制剂（AIs）开辟了一个新时代，以对抗雌激素介导的乳腺癌。尽管有几个优点，但各种不利影响限制了AI的使用。因此，设计具有较少不良影响的选择性AI仍然是一项艰巨而艰巨的工作。在本文中，对类固醇芳香酶抑制剂（SAIs）的定量结构-活性关系（QSAR）的比较研究进行了详细讨论，以深入了解SAIs控制芳香酶抑制活性的结构和理化性质。该研究表明，SAIs应具有较小的形状和尺寸，具有较小的取代基，具有较小的极性和较小的空间效应，并具有较高的疏水性，以具有较高的芳香酶抑制活性。这项研究显然将为药物化学家设计和发现新颖，有效且毒性较小的SAI对抗威胁生命的乳腺癌以及启动乳腺癌药物发现的现代时代提供新思路。