Design, synthesis and biochemical studies of new 7α-allylandrostanes as aromatase inhibitors.
Steroids
; 78(7): 662-9, 2013 Jul.
Article
em En
| MEDLINE
| ID: mdl-23499824
ABSTRACT
Two series of derivatives of 7α-allylandrostenedione, namely its 3-deoxo and 1-ene analogs, were designed and synthesised and their biochemical activity towards aromatase evaluated. In each of these series, the C-17 carbonyl group was further replaced by the hydroxyl and acetoxyl groups. The attained data pointed out that the absence of the C-3 carbonyl group led to a slightly decrease in the inhibitory activity and the introduction of an additional double bond in C-1 revealed to be a very beneficial structural change in the studied compounds (compound 12, IC50 = 0.47 µM, K(i) = 45.00 nM). Furthermore, the relevance of the C-17 carbonyl group in the D-ring as a structural feature required to achieve maximum aromatase inhibitory activity is also observed for this set of derivatives.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Esteroides
/
Inibidores da Aromatase
Limite:
Humans
Idioma:
En
Revista:
Steroids
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Portugal