Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically Active Compounds: A Review
Steroids constitute a unique class of chemical compounds, playing an important role in physiopathological processes, and have high pharmacological interest. Additionally, steroids have been associated with a relatively low toxicity and high bioavailability. Nowadays, multiple steroidal derivatives a...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/7/2032 |
| _version_ | 1797539002496057344 |
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| author | Vanessa Brito Gilberto Alves Paulo Almeida Samuel Silvestre |
| author_facet | Vanessa Brito Gilberto Alves Paulo Almeida Samuel Silvestre |
| author_sort | Vanessa Brito |
| collection | DOAJ |
| description | Steroids constitute a unique class of chemical compounds, playing an important role in physiopathological processes, and have high pharmacological interest. Additionally, steroids have been associated with a relatively low toxicity and high bioavailability. Nowadays, multiple steroidal derivatives are clinically available for the treatment of numerous diseases. Moreover, different structural modifications on their skeleton have been explored, aiming to develop compounds with new and improved pharmacological properties. Thus, steroidal arylidene derivatives emerged as a relevant example of these modifications. This family of compounds has been mainly described as 17β-hydroxysteroid dehydrogenase type 1 and aromatase inhibitors, as well as neuroprotective and anticancer agents. Besides, due to their straightforward preparation and intrinsic chemical reactivity, steroidal arylidene derivatives are important synthetic intermediates for the preparation of other compounds, particularly bearing heterocyclic systems. In fact, starting from arylidenesteroids, it was possible to develop bioactive steroidal pyrazolines, pyrazoles, pyrimidines, pyridines, spiro-pyrrolidines, amongst others. Most of these products have also been studied as anti-inflammatory and anticancer agents, as well as 5α-reductase and aromatase inhibitors. This work aims to provide a comprehensive overview of steroidal arylidene derivatives described in the literature, highlighting their bioactivities and importance as synthetic intermediates for other pharmacologically active compounds. |
| first_indexed | 2024-03-10T12:39:12Z |
| format | Article |
| id | doaj.art-f9741811ce5d42a2b40a8eca321e5c91 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T12:39:12Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-f9741811ce5d42a2b40a8eca321e5c912023-11-21T14:02:08ZengMDPI AGMolecules1420-30492021-04-01267203210.3390/molecules26072032Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically Active Compounds: A ReviewVanessa Brito0Gilberto Alves1Paulo Almeida2Samuel Silvestre3CICS-UBI—Health Sciences Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalCICS-UBI—Health Sciences Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalCICS-UBI—Health Sciences Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalCICS-UBI—Health Sciences Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalSteroids constitute a unique class of chemical compounds, playing an important role in physiopathological processes, and have high pharmacological interest. Additionally, steroids have been associated with a relatively low toxicity and high bioavailability. Nowadays, multiple steroidal derivatives are clinically available for the treatment of numerous diseases. Moreover, different structural modifications on their skeleton have been explored, aiming to develop compounds with new and improved pharmacological properties. Thus, steroidal arylidene derivatives emerged as a relevant example of these modifications. This family of compounds has been mainly described as 17β-hydroxysteroid dehydrogenase type 1 and aromatase inhibitors, as well as neuroprotective and anticancer agents. Besides, due to their straightforward preparation and intrinsic chemical reactivity, steroidal arylidene derivatives are important synthetic intermediates for the preparation of other compounds, particularly bearing heterocyclic systems. In fact, starting from arylidenesteroids, it was possible to develop bioactive steroidal pyrazolines, pyrazoles, pyrimidines, pyridines, spiro-pyrrolidines, amongst others. Most of these products have also been studied as anti-inflammatory and anticancer agents, as well as 5α-reductase and aromatase inhibitors. This work aims to provide a comprehensive overview of steroidal arylidene derivatives described in the literature, highlighting their bioactivities and importance as synthetic intermediates for other pharmacologically active compounds.https://www.mdpi.com/1420-3049/26/7/2032steroidsarylidenesteroidsaldol condensationbioactivityheterocycles |
| spellingShingle | Vanessa Brito Gilberto Alves Paulo Almeida Samuel Silvestre Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically Active Compounds: A Review Molecules steroids arylidenesteroids aldol condensation bioactivity heterocycles |
| title | Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically Active Compounds: A Review |
| title_full | Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically Active Compounds: A Review |
| title_fullStr | Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically Active Compounds: A Review |
| title_full_unstemmed | Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically Active Compounds: A Review |
| title_short | Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically Active Compounds: A Review |
| title_sort | highlights on steroidal arylidene derivatives as a source of pharmacologically active compounds a review |
| topic | steroids arylidenesteroids aldol condensation bioactivity heterocycles |
| url | https://www.mdpi.com/1420-3049/26/7/2032 |
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