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Abstract
A series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified with different phosphate or thiophosphate moieties. The inhibitory properties of the synthesized compounds were tested against human placenta STS. Some of the novel STS inhibitors had good activities against STS. In particular, the bis-(4-oxo-2-(p-tolyl)-4H-chromen-7-yl) hydrogenthiophosphate, 6i had the most potent inhibitory effect with an IC50 value of 3.25 µM as compared to an IC50 value of 8.50 µM for the 2-(4-trifluoromethylphenyl)-chromen-4-one-7-O-sulfamate used as a reference.
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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 8,
pages 450 - 462,
ISSN: 0272-4391 - Language:
- English
- Publication year:
- 2015
- Bibliographic description:
- Kozak W., Daśko M., Masłyk M., Kubiński K., Rachoń J., Demkowicz S.: Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs// DRUG DEVELOPMENT RESEARCH. -Vol. 76, iss. 8 (2015), s.450-462
- DOI:
- Digital Object Identifier (open in new tab) 10.1002/ddr.21281
- Verified by:
- Gdańsk University of Technology
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