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Synthesis and evaluation of geldanamycin-testosterone hybrids

Kuduk SD, Harris TC, Zheng FF, Sepp-Lorenzino L, Ouerfelli Q, Rosen N, Danishefsky SJ

Bioorganic & medicinal chemistry letters, 2000

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.

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