Synthesis and evaluation of geldanamycin-testosterone hybrids

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-06, Vol.10 (11), p.1303-1306
Hauptverfasser:	KUDUK, S. D, HARRIS, C. R, ZHENG, F. F, SEPP-LORENZINO, L, OUERFELLI, Q, ROSEN, N, DANISHEFSKY, S. J
Format:	Artikel
Sprache:	eng
Schlagworte:	Androgen Receptor Antagonists Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Benzoquinones Biological and medical sciences Drug Evaluation Drug Screening Assays, Antitumor General aspects Humans Lactams, Macrocyclic Medical sciences Neoplasms, Hormone-Dependent - metabolism Neoplasms, Hormone-Dependent - pathology Pharmacology. Drug treatments Quinones - chemistry Receptors, Estrogen - metabolism Testosterone - chemistry Tumor Cells, Cultured
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00208-0