Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17β-hydroxysteroid dehydrogenase type 3

被引：45

作者：

Fink, BE

Gavai, AV

Tokarski, JS

Goyal, B

Misra, R

Xiao, HY

Kimball, SD

Han, WC

Norris, D

Spires, TE

You, D

Gottardis, MM

Lorenzi, MV

Vite, GD

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Oncol Chem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Biol, Princeton, NJ 08543 USA

[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Comp Aided Drug Design, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 06期

关键词：

17; beta-HSD3; hydroxysteroid dehydrogenase; androstenedione; tetrahydrodibenzazocine; prostate cancer;

D O I：

10.1016/j.bmcl.2005.12.039

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 17 beta-hydroxysteroid dehydrogenase type 3 (17 beta-HSD3) inhibitors has been identified. These inhibitors, based on a dibenzazocine core, exhibited picomolar to low nanomolar inhibition of 17 beta-HSD3 in cell-free enzymatic as well as in cell-based transcriptional reporter assays. (C) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1532 / 1536

页数：5

共 20 条

[1] CONTROL OF SECRETION AND THE FUNCTION OF C-19-DELTA-5-STEROIDS OF THE HUMAN ADRENAL-GLAND [J].