Substituted 1-[(benzofuran-2-YL)-phenylmethyl]-imidazoles as potent inhibitors of aromatase in vitro and in female rats in vivo

Substituted 1-[(benzofuran-2-YL)-phenylmethyl]-imidazoles as potent inhibitors of aromatase in vitro and in female rats in vivo

Substituted 1-[(benzofuran-2-yl)-phenylmethyl]-imidazoles are a new class of potent aromatase inhibitor with in vitro IC 50 values < 10 nM for certain members using human placental enzyme. At a dose of 2 mg/kg in PMSG-stimulated rats, selected compounds effectively reduce the oestradiol levels by...

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Veröffentlicht in:Journal of steroid biochemistry and molecular biology 1993-03, Vol.44 (4), p.675-676
Hauptverfasser: Whomsley, R., Fernandez, E., Nicholls, P.J., Smith, H.J., Lombardi, P., Pestellini, V.
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Aromatase Inhibitors
Benzofurans - pharmacology
Biological and medical sciences
Estradiol - blood
Female
Gonadotropins, Equine - pharmacology
Hormones. Endocrine system
Humans
Imidazoles - pharmacology
Kinetics
Medical sciences
Microsomes - enzymology
Molecular Structure
Pharmacology. Drug treatments
Placenta - enzymology
Pregnancy
Rats
Structure-Activity Relationship
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Zusammenfassung:Substituted 1-[(benzofuran-2-yl)-phenylmethyl]-imidazoles are a new class of potent aromatase inhibitor with in vitro IC 50 values < 10 nM for certain members using human placental enzyme. At a dose of 2 mg/kg in PMSG-stimulated rats, selected compounds effectively reduce the oestradiol levels by 82–98%.
ISSN:0960-0760
1879-1220
DOI:10.1016/0960-0760(93)90279-6