Non-steroidal aromatase inhibitors based on a biphenyl scaffold: synthesis, in vitro SAR, and molecular modelling.
ChemMedChem
; 3(4): 603-18, 2008 Apr.
Article
en En
| MEDLINE
| ID: mdl-18236493
ABSTRACT
The synthesis and in vitro biological evaluation (JEG-3 cells) of a series of novel and potent aromatase inhibitors, prepared by microwave-enhanced Suzuki cross-coupling methodology, are reported. These compounds possess a biphenyl template incorporated with the haem-ligating triazolylmethyl moiety, either on its own or in combination with other substituent(s) at various positions on the phenyl rings. The most potent aromatase inhibitor reported herein has an IC(50) value of 0.12 nM, although seven of its congeners are also highly potent (IC(50)
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Compuestos de Bifenilo
/
Inhibidores de la Aromatasa
Límite:
Humans
Idioma:
En
Revista:
ChemMedChem
Asunto de la revista:
FARMACOLOGIA
/
QUIMICA
Año:
2008
Tipo del documento:
Article
País de afiliación:
Reino Unido