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Journal article

Design, synthesis, and biological evaluation of new arylamide derivatives possessing sulfonate or sulfamate moieties as steroid sulfatase enzyme inhibitors

Abstract:

A series of new arylamide derivatives possessing terminal sulfonate or sulfamate moieties was designed and synthesized. The target compounds were tested for in vitro inhibitory effects against the steroid sulfatase (STS) enzyme in a cell-free assay system. The free sulfamate derivative 1j was the most active. It inhibited the enzymatic activity by 72.0% and 55.7% at 20 μM and 10 μM, respectively. Compound 1j was further tested for STS inhibition in JEG-3 placental carcinoma cells with high ST...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.bmc.2016.04.040

Authors


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Institution:
University of Oxford
Division:
MSD
Department:
Pharmacology
Role:
Author
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Funding agency for:
Potter, B
Grant:
101010
United Arab Emirates More from this funder
Boehringer Ingelheim More from this funder
Publisher:
Elsevier Publisher's website
Journal:
Bioorganic and Medicinal Chemistry Journal website
Publication date:
2016-04-01
Acceptance date:
2016-04-21
DOI:
ISSN:
1464-3391
Source identifiers:
617148
Keywords:
Pubs id:
pubs:617148
UUID:
uuid:ea9e51a2-e68a-427a-aeea-2c90106fe2f4
Local pid:
pubs:617148
Deposit date:
2016-04-22

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