Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis.
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BORIS DOI
Date of Publication
September 5, 2023
Publication Type
Article
Division/Institute
Author
Wróbel, Tomasz M | |
Mannella, Iole | |
Oliaro-Bosso, Simonetta | |
Nieckarz, Patrycja | |
Therkelsen, Søren | |
Jørgensen, Flemming Steen | |
Pippione, Agnese C | |
Lolli, Marco L | |
Boschi, Donatella | |
Björkling, Fredrik |
Subject(s)
Series
Biomolecules
ISSN or ISBN (if monograph)
2218-273X
Publisher
MDPI
Language
English
Publisher DOI
PubMed ID
37759751
Uncontrolled Keywords
Description
This study reports on the synthesis and evaluation of novel compounds replacing the nitrogen-containing heterocyclic ring on the chemical backbone structure of cytochrome P450 17α-hydroxylase/12,20-lyase (CYP17A1) inhibitors with a phenyl bearing a sulfur-based substituent. Initial screening revealed compounds with marked inhibition of CYP17A1 activity. The selectivity of compounds was thereafter determined against cytochrome P450 21-hydroxylase, cytochrome P450 3A4, and cytochrome P450 oxidoreductase. Additionally, the compounds showed weak inhibitory activity against aldo-keto reductase 1C3 (AKR1C3). The compounds' impact on steroid hormone levels was also assessed, with some notable modulatory effects observed. This work paves the way for developing more potent dual inhibitors specifically targeting CYP17A1 and AKR1C3.
File(s)
File | File Type | Format | Size | License | Publisher/Copright statement | Content | |
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biomolecules-13-01349.pdf | text | Adobe PDF | 3.77 MB | published |