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 referenc...

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Bibliographic Details
Published inFarmaco (Società chimica italiana : 1989) Vol. 49; no. 7-8; pp. 489 - 492
Main Authors HIDA, F, ROBERT, J, LUUDUC, C
Format Journal Article
LanguageEnglish
Published ROME Soc Chimica Italiana 01.07.1994
Subjects
Aromatase Inhibitors
Benzimidazoles - chemical synthesis
Benzimidazoles - pharmacology
Female
Humans
Imidazoles - chemical synthesis
Imidazoles - pharmacology
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
Stereoisomerism
Structure-Activity Relationship
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Summary: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.
ISSN:0014-827X
1879-0569