Synthesis and evaluation of geldanamycin-testosterone hybrids

Authors
Kuduk, SD Harris, CR Zheng, FZF Sepp-Lorenzino, L Ouerfelli, Q Rosen, N Danishefsky, SJ
Citation
Sd. Kuduk et al., Synthesis and evaluation of geldanamycin-testosterone hybrids, BIOORG MED, 10(11), 2000, pp. 1303-1306
Citations number
30
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
11
Year of publication
2000
Pages
1303 - 1306
Database
ISI
SICI code
0960-894X(20000605)10:11<1303:SAEOGH>2.0.ZU;2-N
Abstract
Geldanamycin (GDM) binds to the Hsp90 chaperone protein resulting in the de gradation of several important signaling proteins. A series of GDM-testoste rone 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.