2. Academic Validation
  3. Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors

Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors

  • Bioorg Med Chem Lett. 2009 Dec 15;19(24):6845-50. doi: 10.1016/j.bmcl.2009.10.091.
Vinod D Jadhav 1,  Adam S Duerfeldt,  Brian S J Blagg
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Malott 4070, Lawrence, KS 66045-7562, USA.
PMID: 19896848 DOI: 10.1016/j.bmcl.2009.10.091
Abstract

Bicyclic radester analogues have been synthesized and evaluated for HSP90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic analogues manifesting increased activity versus the five-membered counterparts.

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