The purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulphatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including oestrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability of active hormones for cancer cells, causing a positive therapeutic effect. Herein, we report examples of novel STS inhibitors based on steroidal and nonsteroidal cores that contain various functional groups (e.g. sulphamate and phosphorus moieties) and halogen atoms, which may potentially be used in therapies for hormone-dependent cancers. The presented work also includes examples of multitargeting agents with STS inhibitory activities. Furthermore, the fundamental discoveries in the development of the most promising drug candidates exhibiting STS inhibitory activities are highlighted.

中文翻译：

---

类固醇硫酸酯酶抑制剂开发的最新进展-过去十年中新颖且最有前途的化合物的实例。

本文的目的是概述新型甾体硫酸酯酶（STS）抑制剂的合成最新进展。STS是活性激素（包括雌激素和雄激素）的生物合成中的关键酶，因此代表了激素依赖性癌症治疗方法的发展中极具吸引力的分子靶标。抑制STS可能有效降低癌细胞中活性激素的利用率，从而产生积极的治疗效果。本文中，我们报告了基于类固醇和非类固醇核心的新型STS抑制剂的实例，这些抑制剂包含各种官能团（例如氨基磺酸盐和磷部分）和卤素原子，它们可能会用于激素依赖性癌症的治疗中。提出的工作还包括具有STS抑制活性的多靶标药物的实例。此外，突出显示了最有前途的候选药物具有STS抑制活性的发展中的基本发现。