Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
Bioorg Med Chem Lett
; 17(17): 4824-8, 2007 Sep 01.
Article
em En
| MEDLINE
| ID: mdl-17614275
ABSTRACT
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe the syntheses of cyclopentanone and cyclohexanone intermediates for SAR studies of the C-ring on the benzopyran scaffold. Modification of the C-ring disrupts binding to ERalpha, thus improving ERbeta selectivity up to 100-fold. X-ray cocrystal structures confirm previously observed binding modes.
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Base de dados:
MEDLINE
Assunto principal:
Benzopiranos
/
Química Farmacêutica
/
Moduladores Seletivos de Receptor Estrogênico
/
Cicloexanonas
/
Ciclopentanos
/
Receptor beta de Estrogênio
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article