Synthesis and evaluation of geldanamycin-testosterone hybrids Journal Article


Authors: Kuduk, S. D.; Harris, C. R.; Zheng, F. F.; Sepp-Lorenzino, L.; Ouerfelli, O.; Rosen, N.; Danishefsky, S. J.
Article Title: Synthesis and evaluation of geldanamycin-testosterone hybrids
Abstract: 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.
Keywords: antineoplastic agents; drug inhibition; breast cancer; protein degradation; cell line; drug potency; drug screening assays, antitumor; tumor cells, cultured; drug selectivity; drug synthesis; prostate cancer; hybrid protein; colon cancer; cancer cell; quinones; androgen receptor; receptors, estrogen; drug cytotoxicity; receptors, androgen; testosterone; drug binding; benzoquinones; lactams, macrocyclic; neoplasms, hormone-dependent; geldanamycin; chaperone; drug evaluation; humans; article
Journal Title: Bioorganic & Medicinal Chemistry Letters
Volume: 10
Issue: 11
ISSN: 0960-894X
Publisher: Pergamon-Elsevier Science Ltd  
Date Published: 2000-06-05
Start Page: 1303
End Page: 1306
Language: English
DOI: 10.1016/s0960-894x(00)00208-0
PUBMED: 10866406
PROVIDER: scopus
DOI/URL:
Notes: Export Date: 18 November 2015 -- Source: Scopus
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MSK Authors
  1. Neal Rosen
    364 Rosen
  2. Fuzhong F Zheng
    11 Zheng
  3. Scott D Kuduk
    21 Kuduk
  4. Christina R Harris
    12 Harris