Laboratory of Medicinal Chemistry, Department of Pharmacy, University of Patras, Patras GR-26500, Greece.
Laboratory of Medicinal Chemistry, Department of Pharmacy, University of Patras, Patras GR-26500, Greece.
Bioorg Chem. 2022 Nov;128:106089. doi: 10.1016/j.bioorg.2022.106089. Epub 2022 Aug 11.
Prostate cancer (PCa) remains a serious type of cancer for men worldwide. The majority of new PCa cases are associated with androgen receptor (AR) hyperactivity. Various AR-targeting molecules that suppress its activity have been discovered. In this review, we present the already marketed antiandrogens and a selection of structurally and chemically interesting AR-targeting compounds, from a pharmacochemical perspective. Focus has been placed on the applied design approaches, structural evolution and structure-activity relationships of the most prominent compound classes. Passing from the traditional steroidal AR antagonists to the modern AR-targeting proteolysis targeting chimeras (PROTACs), we intend to provide a comprehensive overview on AR-targeting molecules for PCa treatment.
前列腺癌（PCa）仍然是全世界男性面临的一种严重癌症。大多数新的 PCa 病例与雄激素受体（AR）过度活跃有关。已经发现了各种抑制其活性的 AR 靶向分子。在这篇综述中，我们从药理学的角度介绍了已经上市的抗雄激素药物和一些结构和化学上有趣的 AR 靶向化合物。重点放在了应用设计方法、最突出的化合物类别结构演变和构效关系上。从传统的甾体 AR 拮抗剂到现代的 AR 靶向蛋白水解靶向嵌合体（PROTACs），我们旨在提供一个关于用于治疗 PCa 的 AR 靶向分子的全面概述。
