取代的1-[(苯并呋喃-2-基)-苯基甲基]-咪唑类化合物作为体外和雌性大鼠体内强效芳香化酶抑制剂
Substituted 1-[benzofuran-2-yl)-phenylmethyl]-imidazoles as potent inhibitors of aromatase in vitro and in female rats in vivo.
作者信息
Whomsley R, Fernandez E, Nicholls P J, Smith H J, Lombardi P, Pestellini V
机构信息
Welsh School of Pharmacy, U.W.C.C., Cardiff.
出版信息
J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):675-6. doi: 10.1016/0960-0760(93)90279-6.
PMID:8476782
Abstract
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%.
摘要
取代的1-[(苯并呋喃-2-基)-苯基甲基]-咪唑是一类新型强效芳香酶抑制剂，某些成员对人胎盘酶的体外IC50值<10 nM。在PMSG刺激的大鼠中，以2 mg/kg的剂量给药，所选化合物可有效降低雌二醇水平82-98%。
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