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.