[en] 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.
Disciplines :
Immunology & infectious disease Oncology
Author, co-author :
Agouridas, Vangelis
Magnier, Emmanuel
Blazejewski, Jean-Claude
Laïos, Ioanna
Cleeren, Anny
Nonclercq, Denis ; Université de Mons > Faculté de Médecine et de Pharmacie > Service d'Histologie
Laurent, Guy ; Université de Mons > Faculté de Médecine et de Pharmacie > Histologie
Leclercq, Guy
Language :
English
Title :
Effect of fluorination on the pharmacological profile of 11beta isomers of fulvestrant in breast carcinoma cells
Publication date :
12 February 2009
Journal title :
Journal of Medicinal Chemistry
ISSN :
0022-2623
Publisher :
American Chemical Society, United States - District of Columbia
Volume :
52
Issue :
3
Pages :
883-887
Peer reviewed :
Peer Reviewed verified by ORBi
Research unit :
M118 - Histologie
Research institute :
R550 - Institut des Sciences et Technologies de la Santé
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