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3-HYDROXY-19-NOR-17-ALPHA-PREGNA-1,3,5(10)-TRIENE-21,17-BETA-CARBOLACTONE AS INHIBITOR OF 17-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-2

被引：12
作者：
AUGER, S
LUUTHE, V
SAM, KM
POIRIER, D
机构：
[1] CHU LAVAL,RES CTR,DIV MED CHEM,MOLEC ENDOCRINOL LAB,QUEBEC CITY G1V 4G2,PQ,CANADA
[2] UNIV LAVAL,QUEBEC CITY G1V 4G2,PQ,CANADA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 16期
关键词：
D O I：
10.1016/S0960-894X(01)80560-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Introducing a spiro-gamma-lactone at position 17 of an estradiol nucleus provokes a potent inhibition of 17 beta-hydroxysteroid dehydrogenase (17 beta-HSD) type 2. Synthesis of such a compound, namely 6 (3-hydroxy-19-nor-17 alpha-pregna-1,3,5(10)-triene-21,17 beta-carbolactone), was performed in five steps, starting with estrone. Inhibition analysis of this compound, the first inhibitor of 17 beta-HSD, using human placental microsomes and 4-androstene-3,17-dione as substrate shows a Ki value of 0.25 mu M.
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页码：2045 / 2048
页数：4
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