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...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2020-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/14756366.2020.1758692 |
| _version_ | 1818650422493052928 |
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| author | Mateusz Daśko Sebastian Demkowicz Karol Biernacki Olga Ciupak Witold Kozak Maciej Masłyk Janusz Rachon |
| author_facet | Mateusz Daśko Sebastian Demkowicz Karol Biernacki Olga Ciupak Witold Kozak Maciej Masłyk Janusz Rachon |
| author_sort | Mateusz Daśko |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-17T01:49:58Z |
| format | Article |
| id | doaj.art-f089a2247d0c42ee9b6e9c28a518045c |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-12-17T01:49:58Z |
| publishDate | 2020-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-f089a2247d0c42ee9b6e9c28a518045c2022-12-21T22:08:06ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742020-01-013511163118410.1080/14756366.2020.17586921758692Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decadeMateusz Daśko0Sebastian Demkowicz1Karol Biernacki2Olga Ciupak3Witold Kozak4Maciej Masłyk5Janusz Rachon6Department of Inorganic Chemistry, Faculty of Chemistry, Gdansk University of TechnologyDepartment of Organic Chemistry, Faculty of Chemistry, Gdansk University of TechnologyDepartment of Organic Chemistry, Faculty of Chemistry, Gdansk University of TechnologyDepartment of Organic Chemistry, Faculty of Chemistry, Gdansk University of TechnologyDepartment of Physical Chemistry, Faculty of Chemistry, University of GdanskDepartment of Molecular Biology, Faculty of Biotechnology and Environment Sciences, The John Paul II Catholic University of LublinDepartment of Organic Chemistry, Faculty of Chemistry, Gdansk University of TechnologyThe 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.http://dx.doi.org/10.1080/14756366.2020.1758692steroid sulphatasests inhibitorssteroidsmultitargeting agents |
| spellingShingle | Mateusz Daśko Sebastian Demkowicz Karol Biernacki Olga Ciupak Witold Kozak Maciej Masłyk Janusz Rachon Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade Journal of Enzyme Inhibition and Medicinal Chemistry steroid sulphatase sts inhibitors steroids multitargeting agents |
| title | Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade |
| title_full | Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade |
| title_fullStr | Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade |
| title_full_unstemmed | Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade |
| title_short | Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade |
| title_sort | recent progress in the development of steroid sulphatase inhibitors examples of the novel and most promising compounds from the last decade |
| topic | steroid sulphatase sts inhibitors steroids multitargeting agents |
| url | http://dx.doi.org/10.1080/14756366.2020.1758692 |
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