Synthesis and evaluation of geldanamycin-testosterone hybrids
Antineoplastic Combined Chemotherapy Protocols
HSP90 Heat-Shock Proteins
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.