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.
authors.affiliation: Departement of Medicine, Sloan-Kettering Institute for Cancer Research, New York, NY 10021, USA.
authors.forename: S D
authors.initials: SD
authors.lastname: Kuduk
authors.forename: T C
authors.initials: TC
authors.lastname: Harris
authors.forename: F F
authors.initials: FF
authors.lastname: Zheng
authors.forename: L
authors.initials: L
authors.lastname: Sepp-Lorenzino
authors.forename: Q
authors.initials: Q
authors.lastname: Ouerfelli
authors.forename: N
authors.initials: N
authors.lastname: Rosen
authors.forename: S J
authors.initials: SJ
authors.lastname: Danishefsky
mesh_terms: D059002:Androgen Receptor Antagonists; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D016227:Benzoquinones; D004341:Drug Evaluation; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D047029:Lactams, Macrocyclic; D009376:Neoplasms, Hormone-Dependent / Q000378:metabolism / Q000473:pathology; D011809:Quinones / Q000737:chemistry*; D011960:Receptors, Estrogen / Q000378:metabolism; D013739:Testosterone / Q000737:chemistry*; D014407:Tumor Cells, Cultured
chemical_list: D059002:Androgen Receptor Antagonists; D000970:Antineoplastic Agents; D016227:Benzoquinones; D047029:Lactams, Macrocyclic; D011809:Quinones; D011960:Receptors, Estrogen; D013739:Testosterone; C001277:geldanamycin