Recent progress in the development of steroid sulphatase inhibitors - examples of the novel and most promising compounds from the last decade

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 mo...

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Bibliographic Details
Published in:Journal of enzyme inhibition and medicinal chemistry 2020-01, Vol.35 (1), p.1163-1184
Main Authors: Daśko, Mateusz, Demkowicz, Sebastian, Biernacki, Karol, Ciupak, Olga, Kozak, Witold, Masłyk, Maciej, Rachon, Janusz
Format: Article
Language:English
Subjects:
Androgens
Drug development
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Estrogens
Hormones
Humans
Models, Molecular
Molecular Structure
multitargeting agents
Phosphorus
Review
Steroid sulphatase
steroids
Steryl-Sulfatase - antagonists & inhibitors
Steryl-Sulfatase - chemistry
Steryl-Sulfatase - metabolism
STS inhibitors
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Summary: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.
ISSN:1475-6366
1475-6374
1475-6374
DOI:10.1080/14756366.2020.1758692