Synthesis and evaluation of benzimidazole and imidazole compounds as potential aromatase inhibitors.
Several series of benzimidazole and imidazole derivatives have been synthesized and their biological activity evaluated. Their ability to inhibit human placental aromatase activity was tested in vitro. Ten of the tested compounds are more active towards aromatase than aminoglutethimide, the reference molecule. The most active compound XI is five times more potent in the same system. Compounds bearing an aryl group substituted by one or two halogen atom(s) (fluorine or chlorine) in position 4 or 2,4 respectively have also the most interesting activity.
Hida
F
F
Laboratoire de Chimie-Pharmacie, C.N.R.S. URA 1287, Faculté de Pharmacie de Grenoble Université Joseph-Fourier Grenoble, La Tronche, France.
Robert
J
J
Luu-Duc
C
C
D047072:Aromatase Inhibitors; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D047072:Aromatase Inhibitors; D001562:Benzimidazoles; D007093:Imidazoles