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.

引用

页码：2045 / 2048

页数：4

共 18 条

[1]

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[2]

AUGER S, 1993, ANN ACFAS, V61, P109

[3] 17-BETA-HYDROXYSTEROID AND 20-ALPHA-HYDROXYSTEROID DEHYDROGENASE-ACTIVITIES OF HUMAN PLACENTAL MICROSOMES - KINETIC EVIDENCE FOR 2 ENZYMES DIFFERING IN SUBSTRATE-SPECIFICITY [J].