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2-difluoromethoxy-substituted estratriene sulfamates: synthesis, anti-proliferative sar, anti-tubulin activity and steroid sulfatase inhibition

Abstract:

2-Difluoromethoxyestratriene derivatives were designed to improve potency and in vivo stability of the drug candidate 2-methoxyestradiol (2ME2). Compound evaluation in vitro against the proliferation of MCF-7 and MDA MB-231 breast cancer cells, as inhibitors of tubulin polymerisation and also steroid sulfatase (STS) both in cell lysates and in whole cells, showed promising activities. In antiproliferative assays 2-difluoromethoxyestradiol was less potent than 2ME2, but its sulfamates were oft...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1002/cmdc.202200408

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More by this author
Institution:
University of Oxford
Division:
MSD
Department:
Pharmacology
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
Pharmacology
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
Pharmacology
Role:
Author
Publisher:
Wiley
Journal:
CheMedChem More from this journal
Volume:
17
Issue:
23
Article number:
e202200408
Publication date:
2022-09-15
Acceptance date:
2022-09-15
DOI:
EISSN:
1860-7187
ISSN:
1860-7179
Language:
English
Keywords:
Pubs id:
1278994
Local pid:
pubs:1278994
Deposit date:
2022-09-16

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