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Abstract
In the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were tested on STS isolated from human placenta and led to two compounds of interest, 5a and 5d with IC50 values of 28.0 and 22.1 mM, respectively and that had interesting new binding modes in the STS active site. Drug Dev Res 76 : 94–104, 2015.
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Authors (6)
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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:
-
DRUG DEVELOPMENT RESEARCH
no. 76,
edition 2,
pages 94 - 104,
ISSN: 0272-4391 - Language:
- English
- Publication year:
- 2015
- Bibliographic description:
- Demkowicz S., Kozak W., Daśko M., Masłyk M., Kubiński K., Rachoń J.: Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors// DRUG DEVELOPMENT RESEARCH. -Vol. 76, iss. 2 (2015), s.94-104
- DOI:
- Digital Object Identifier (open in new tab) 10.1002/ddr.21245
- Verified by:
- Gdańsk University of Technology
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