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Titolo:
First attachment of the stable organometallic moiety [ Re(CO)(3)(eta(5)-C5H4-C C-)] at position 11 beta of oestradiol. Biochemical behaviour of the complex
Autore:
Morel, P; Top, S; Vessieres, A; Stephan, E; Laios, I; Leclercq, G; Jaouen, G;
Indirizzi:
Ecole Natl Super Chim Paris, CNRS, UMR 7576, Lab Chim Organomet, F-75231 Paris 05, France Ecole Natl Super Chim Paris Paris France 05 et, F-75231 Paris 05, France Inst Jules Bordet, Lab Canc Mammaire, B-1000 Brussels, Belgium Inst Jules Bordet Brussels Belgium B-1000 aire, B-1000 Brussels, Belgium
Titolo Testata:
COMPTES RENDUS DE L ACADEMIE DES SCIENCES SERIE II FASCICULE C-CHIMIE
fascicolo: 3, volume: 4, anno: 2001,
pagine: 201 - 205
SICI:
1387-1609(200103)4:3<201:FAOTSO>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
STEROIDAL AFFINITY LABELS; ESTROGEN-RECEPTOR; ESTRADIOL DERIVATIVES; BIOORGANOMETALLIC CHEMISTRY; RADIOPHARMACEUTICALS; ANTAGONISM; COMPLEXES;
Keywords:
steroid; metallocene; hormone; rhenium; estradiol; estrogen receptor; SERM (specific estrogen receptor modulator);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Citazioni:
34
Recensione:
Indirizzi per estratti:
Indirizzo: Jaouen, G Ecole Natl Super Chim Paris, CNRS, UMR 7576, Lab Chim Organomet,11 Rue Pierre & Marie Curie, F-75231 Paris 05, France Ecole Natl Super Chim Paris 11 Rue Pierre & Marie Curie Paris France 05
Citazione:
P. Morel et al., "First attachment of the stable organometallic moiety [ Re(CO)(3)(eta(5)-C5H4-C C-)] at position 11 beta of oestradiol. Biochemical behaviour of the complex", CR AC S IIC, 4(3), 2001, pp. 201-205

Abstract

We present here the 9-step synthesis of 10, the first rhenium organometallic complex of oestradiol substituted at the 11 beta position. This hormone retains acceptable binding affinity for the oestradiol receptor at 0 degreesC (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. (C) 2001 Academie des sciences / Editions scientifiques et medicales Elsevier SAS.

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Documento generato il 20/01/21 alle ore 03:04:03