AI Article Synopsis
- The synthesis of an 11beta isomer of the steroidal antiestrogen fulvestrant has been described.
- Partial fluorination of this new isomer created a compound that retains strong antiproliferative effects on MCF-7 breast cancer cells.
- Interestingly, this fluorinated compound does not down-regulate the estrogen receptor alpha, indicating that this receptor down-regulation may not be essential for the anti-tumor effects of steroidal antiestrogens.
Article Abstract
We describe the synthesis of an 11beta isomer 3 of the steroidal antiestrogen fulvestrant 2. Partial fluorination of the 11beta side chain in 3 leads to 4, which still shows strong antiproliferative activity on MCF-7 cells. However, unlike 2 and 3, compound 4 fails to down-regulate estrogen receptor alpha (ERalpha). This result suggests that ERalpha down-regulation is not a sine qua non condition for the antitumor activity of steroidal antiestrogens.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm801154q | DOI Listing |
Publication Analysis
Top Keywords
fluorination pharmacological
4
pharmacological profile
4
profile 11beta
4
11beta isomers
4
isomers fulvestrant
4
fulvestrant breast
4
breast carcinoma
4
carcinoma cells
4
cells describe
4
describe synthesis
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!