Synthesis and sulfatase inhibitory activities of (E)- and (Z)-4-hydroxytamoxifen sulfamates

被引：22

作者：

Chu, GH

Peters, A

Selcer, KW

Li, PK ^{[1
]}

机构：

[1] Duquesne Univ, Mylan Sch Pharm, Dept Med Chem & Pharmaceut, Pittsburgh, PA 15282 USA

[2] Duquesne Univ, Bayer Sch Nat & Environm Sci, Dept Biol, Pittsburgh, PA 15282 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(98)00707-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the development of (E)- and (Z)-4-hydroxytamoxifen sulfamates as estrone sulfatase inhibitors, potential therapeutic agents for the treatment of breast cancer. Both compounds competitively inhibit estrone sulfatase isolated from rat liver with apparent K-i of 35.9 mu M for (E)-4-hydroxytamoxifen sulfamate and an apparent K-i of > 500 mu M for the (Z) isomer. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：141 / 144

页数：4

共 22 条

[1]

DUNCAN L, 1993, CANCER RES, V53, P298

[2]

ELGER W, 1995, J STEROID BIOCHEM, V55, P396

[3] New highly stereoselective synthesis of (Z)-4-Hydroxytamoxifen and (Z)-4-hydroxytoremifene via McMurry reaction [J].