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C-3 and C-4 substituted bicyclic coumarin sulfamates are potent steroid sulfatase inhibitors

Abstract:

Synthetic routes to potent bicyclic nonsteroidal sulfamate-based active-site-directed inhibitors of the enzyme steroid sulfatase (STS), an emerging target in the treatment of postmenopausal hormone-dependent diseases, including breast cancer, are described. Sulfamate analogs 9–27 and 28–46 of the core in vivo active two-ring coumarin template, modified at the 4- and 3-positions, respectively, were synthesized to expand structure–activity relationships. α-Alkylacetoacetates were used to synthe...

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Publication status:
Published
Peer review status:
Peer reviewed

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Institution:
University of Oxford
Division:
MSD
Department:
Pharmacology
Role:
Author
ORCID:
0000-0003-3255-9135
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Name:
Engineering and Physical Sciences Research Council
Publisher:
American Chemical Society
Journal:
ACS Omega More from this journal
Volume:
3
Issue:
9
Pages:
10748–10772
Publication date:
2018-09-06
Acceptance date:
2018-08-16
DOI:
EISSN:
2470-1343
Pubs id:
pubs:907555
UUID:
uuid:e8d2fa2c-c4e3-4f54-9d1d-5c0ed881d865
Local pid:
pubs:907555
Source identifiers:
907555
Deposit date:
2018-08-16

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