SUBSTITUTED 1-[(BENZOFURAN-2-YL)-PHENYLMETHYL]-IMIDAZOLES AS POTENT INHIBITORS OF AROMATASE INVITRO AND IN FEMALE RATS INVIVO

被引:45
作者
WHOMSLEY, R
FERNANDEZ, E
NICHOLLS, PJ
SMITH, HJ
LOMBARDI, P
PESTELLINI, V
机构
[1] UWCC,WELSH SCH PHARM,CARDIFF,WALES
[2] MENARINI SUD,I-0040 POMEZIA,ITALY
[3] A MENARINI IND FARMACEUT RIUNITE,I-50131 FLORENCE,ITALY
关键词
D O I
10.1016/0960-0760(93)90279-6
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 2mg/kg in PMSG-stimulated rats, selected compounds effectively reduce the oestradiol levels by 82-98%.
引用
收藏
页码:675 / 676
页数:2
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