Synthesis and evaluation of geldanamycin-testosterone hybrids

Bioorg Med Chem Lett. 2000 Jun 5;10(11):1303-6. doi: 10.1016/s0960-894x(00)00208-0.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Androgen Receptor Antagonists
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Benzoquinones
  • Drug Evaluation
  • Drug Screening Assays, Antitumor
  • Humans
  • Lactams, Macrocyclic
  • Neoplasms, Hormone-Dependent / metabolism
  • Neoplasms, Hormone-Dependent / pathology
  • Quinones / chemistry*
  • Receptors, Estrogen / metabolism
  • Testosterone / chemistry*
  • Tumor Cells, Cultured


  • Androgen Receptor Antagonists
  • Antineoplastic Agents
  • Benzoquinones
  • Lactams, Macrocyclic
  • Quinones
  • Receptors, Estrogen
  • Testosterone
  • geldanamycin