• Citer

Effect of fluorination on the pharmacological profile of 11β isomers of fulvestrant in breast carcinoma cells

par Agouridas, Vangelis;Magnier, Emmanuel;Blazejewski, Jean-Claude;Laïos, Ioanna;Cleeren, Anny ;Nonclercq, Denis;Laurent, Guy ;Leclercq, Guy
Référence Journal of medicinal chemistry, 52, 3, page (883-887)
Publication Publié, 2009-02

Article révisé par les pairs

• Détails
• Contenu

Résumé :

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.