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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