Journal article
2-difluoromethoxy-substituted estratriene sulfamates: synthesis, anti-proliferative sar, anti-tubulin activity and steroid sulfatase inhibition
- Abstract:
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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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- Files:
-
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(Preview, Accepted manuscript, pdf, 956.2KB, Terms of use)
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- Publisher copy:
- 10.1002/cmdc.202200408
Authors
Bibliographic Details
- 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:
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1860-7187
- ISSN:
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1860-7179
Item Description
- Language:
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English
- Keywords:
- Pubs id:
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1278994
- Local pid:
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pubs:1278994
- Deposit date:
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2022-09-16
Terms of use
- Copyright holder:
- Wiley
- Copyright date:
- 2022
- Rights statement:
- © 2022 Wiley-VCH GmbH.
- Notes:
- This is the accepted manuscript version of the article. The final version is available online from Wiley at: https://doi.org/10.1002/cmdc.202200408
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