Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
Bioorg Med Chem Lett
; 16(4): 821-4, 2006 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-16307879
ABSTRACT
The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tamoxifeno
/
Receptores de Estrogênio
/
Receptores Citoplasmáticos e Nucleares
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2006
Tipo de documento:
Article