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 IC50 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%.
Whomsley
R
R
Welsh School of Pharmacy, U.W.C.C., Cardiff.
Fernandez
E
E
Nicholls
P J
PJ
Smith
H J
HJ
Lombardi
P
P
Pestellini
V
V
D000818:Animals; D047072:Aromatase Inhibitors; D001572:Benzofurans / Q000494:pharmacology*; D004958:Estradiol / Q000097:blood*; D005260:Female; D006064:Gonadotropins, Equine / Q000494:pharmacology; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology*; D007700:Kinetics; D008861:Microsomes / Q000201:enzymology*; D015394:Molecular Structure; D010920:Placenta / Q000201:enzymology*; D011247:Pregnancy; D051381:Rats; D013329:Structure-Activity Relationship
D047072:Aromatase Inhibitors; D001572:Benzofurans; D006064:Gonadotropins, Equine; D007093:Imidazoles; D004958:Estradiol