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ID: ALA1131689

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of geldanamycin-estradiol hybrids.

Authors: Kuduk SD, Zheng FF, Sepp-Lorenzino L, Rosen N, Danishefsky SJ.

Abstract: Geldanamycin (GDM) binds to the Hsp90 chaperone protein and causes the degradation of several important signalling proteins. A series of novel estradiol-geldanamycin hybrids has been synthesized and evaluated for their ability to induce the selective degradation of the estrogen receptor (ER). The hybrid compounds are active and more selective than the parent causing degradation of ER and HER2, but not other GDM targets.

CiteXplore: 10340605

DOI: 10.1016/s0960-894x(99)00185-7