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Synthesis and biological evaluation of 4-imidazolylflavans as nonsteroidal aromatase inhibitors

Tipo de material: TextoTextoSeries ; Bioorganic Chemistry, 32(6), p.494-503, 2004Trabajos contenidos:
  • Pouget, C
  • Yahiaoui,S
  • Fagnere, C
  • Habrioux, G
  • Chulia, A.J
Tema(s): Recursos en línea: Resumen: A series of 4-imidazolylflavans having a variety of substituents on the 2-phenyl ring was synthesized and investigated for their inhibitory effect against aromatase. Structure-activity relationships of these compounds were determined. An additional chlorine atom or a cyano group at the 40 position did not enhance aromatase inhibition as well as a 30-hydroxyl group. The influence of an additional 40-hydroxyl group depends on the substitution pattern of A ring. Among these molecules, 40-hydroxy-4-imidazolyl-7-methoxyflavan is only 2.2-fold less active than the letrozole (as assessed by IC50 values). Letrozole is used as the first-line therapy for metastatic breast cancer.
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A series of 4-imidazolylflavans having a variety of substituents on the 2-phenyl ring was synthesized and investigated for their inhibitory effect against aromatase. Structure-activity relationships of these compounds were determined. An additional chlorine atom or a cyano group at the 40 position did not enhance aromatase inhibition as well as a 30-hydroxyl group. The influence of an additional 40-hydroxyl group depends on the substitution pattern of A ring. Among these molecules, 40-hydroxy-4-imidazolyl-7-methoxyflavan is only 2.2-fold less active than the letrozole (as assessed by IC50 values). Letrozole is used as the first-line therapy for metastatic breast cancer.

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