16-ALPHA-PROPYL DERIVATIVES OF ESTRADIOL AS INHIBITORS OF 17-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-1

被引：20

作者：

SAM, KM

BOIVIN, RP

AUGER, S

POIRIER, D

机构：

[1] CHU LAVAL,RES CTR,MOLEC ENDOCRINOL LAB,DIV MED CHEM,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 / 17期

关键词：

D O I：

10.1016/S0960-894X(01)80115-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of eight 16 alpha-propyl derivatives of estradiol is described, and structure-activity relationships are discussed. Potent inhibitors of cytosolic 17 beta-hydroxysteroid dehydrogenase of human placenta (type 1) can be obtained when a good leaving group is located at the end of a 16 alpha-propyl side chain; the 16 alpha-(iodopropyl)-estradiol (7) and 16 alpha-(bromopropyl)-estradiol (6) gave the best irreversible inhibitions of 17 beta-HSD type 1, with IC50 values of 0.42 and 0.46 mu M, respectively.

引用

页码：2129 / 2132

页数：4

共 12 条

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