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First attachment of the stable organometallic moiety [Re(CO)3(η5-C5H4-C≡C-)] at position 11ß of oestradiol. Biochemical behaviour of the complex

par Morel, Pierre ;Top, Siden;Vessières, Anne;Stéphan, Élie E.;Laïos, Ioanna;Leclercq, Guy ;Jaouen, Gérard
Référence Comptes Rendus de l'Academie des Sciences - Series IIc: Chemistry, 4, 3, page (201-205)
Publication Publié, 2001

Article révisé par les pairs

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Résumé :

We present here the 9-step synthesis of 10, the first rhenium organometallic complex of oestradiol substituted at the 11β position. This hormone retains acceptable binding affinity for the oestradiol receptor at 0 °C (11%) while its partition coefficient shows it is more lipophilic than oestradiol. The test of its agonist/antagonist activity on oestrogen receptor positive cell line (MVLN) shows it acts as a potent agonist almost as strong as oestradiol itself. © 2001 Académie des sciences/Éditions scientifiques et médicales Elsevier SAS.