11 beta-substituted estradiol derivatives. 2. Potential carbon-11- and iodine-labeled probes for the estrogen receptor.
J Med Chem
; 38(14): 2774-9, 1995 Jul 07.
Article
en En
| MEDLINE
| ID: mdl-7629815
ABSTRACT
Four new classes of 11 beta-substituted estradiol and estriol derivatives (cyanoalkyl, ethynyl, propynyl, and iodovinyl) have been synthesized, and their binding affinity for the estrogen receptor has been evaluated. The binding affinity values indicate that the estrogen receptor has tolerance for estradiol derivatives bearing 11 beta-groups whose size, rigidity, and polarity are limited. The estradiol derivatives have higher affinity than the estriol derivatives. The potential of these agents as imaging agent for estrogen receptor-positive breast tumors is discussed. On the basis of the results of this and a previously reported study (Napolitano, E.; Fiaschi, R.; Carlson, K. E.; Katzenellenbogen, J. A. 11 beta-Substituted Estradiol Derivatives, Potential High-Affinity Carbon-11-Labeled Probes for the Estrogen Receptor A Structure-Affinity Relationship Study. J. Med. Chem. 1995, 38, 429-434), a general strategy for designing high-affinity probes for the estrogen receptor is proposed.
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Banco de datos:
MEDLINE
Asunto principal:
Sondas Moleculares
/
Receptores de Estrógenos
/
Estradiol
Límite:
Animals
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
1995
Tipo del documento:
Article
País de afiliación:
Italia