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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
Abstract
In the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic STS assay; both had IC50 values of 0.27 μM (the IC50 value of coumarin-7-O-sulfamate is 3.5 μM, used as a reference).
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Authors (8)
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Maciej Masłyk
- The John Paul II Catholic University of Lublin Department of Molecular Biology, Faculty of Biotechnology and Environment Sciences
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Konrad Kubiński
- The John Paul II Catholic University of Lublin Department of Molecular Biology, Faculty of Biotechnology and Environment Sciences
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Details
- Category:
- Articles
- Type:
- artykuł w czasopiśmie wyróżnionym w JCR
- Published in:
-
Chemical Biology & Drug Design
no. 87,
pages 233 - 238,
ISSN: 1747-0277 - Language:
- English
- Publication year:
- 2016
- Bibliographic description:
- Demkowicz S., Daśko M., Kozak W., Krawczyk K., Witt D., Masłyk M., Kubiński K., Rachoń J.: Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors// Chemical Biology & Drug Design. -Vol. 87, nr. 2 (2016), s.233-238
- DOI:
- Digital Object Identifier (open in new tab) 10.1111/cbdd.12652
- Verified by:
- Gdańsk University of Technology
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