Synthesis and evaluation of geldanamycin-estradiol hybrids

被引：108

作者：

Kuduk, SD

Zheng, FF

Sepp-Lorenzino, L

Rosen, N

Danishefsky, SJ

机构：

[1] Sloan Kettering Inst Canc Res, Bioorgan Chem Lab, New York, NY 10021 USA

[2] Sloan Kettering Inst Canc Res, Cell Biol Program, Dept Med, New York, NY 10021 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(99)00185-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Geldanamycin (GDM) binds to the Hsp90 chaperone protein and causes the degradation of several important signalling proteins. A series of novel estradiol-geldanamycin hybrids has been synthesized and evaluated for their ability to induce the selective degradation of the estrogen receptor (ER). The hybrid compounds are active and more selective than the parent causing degradation of ER and HER2, but not other GDM targets. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1233 / 1238

页数：6

共 20 条

[1] The estradiol pharmacophore: Ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site [J].