Synthesis and evaluation of geldanamycin-testosterone hybrids

被引：84

作者：

Kuduk, SD

Harris, CR

Zheng, FZF

Sepp-Lorenzino, L

Ouerfelli, Q

Rosen, N

Danishefsky, SJ

机构：

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

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

[3] Sloan Kettering Inst Canc Res, Dept Med, Program Cellular Biochem & Biophys, New York, NY 10021 USA

[4] Columbia Univ, Dept Chem, New York, NY 10027 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(00)00208-0

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 resulting in the degradation of several important signaling proteins. A series of GDM-testosterone linked hybrids has been synthesized and evaluated for activity against prostate cancer cell lines. The hybrid with the greatest activity exhibits potent and selective cytotoxicity against prostate cancer cells containing the androgen receptor. (C) 2000 Elsevier Science Ltd. All rights reserved.

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收藏

页码：1303 / 1306

页数：4

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