Triazole containing novobiocin and biphenyl amides as Hsp90 C-terminal inhibitors

Jinbo Zhao, Huiping Zhao, Jessica A. Hall, Douglas Brown, Eileen Brandes, Joseph Bazzill, Patrick T. Grogan, Chitra Subramanian, George Vielhauer, Mark S. Cohen, Brian S.J. Blagg

Research output: Contribution to journalArticlepeer-review


Hsp90 C-terminal inhibitors are advantageous for the development of new cancer chemotherapeutics due to their ability to segregate client protein degradation from induction of the prosurvival heat shock response, which is a major detriment associated with Hsp90 N-terminal inhibitors under clinical investigation. Based upon prior SAR trends, a 1,2,3-triazole side chain was placed in lieu of the aryl side chain and attached to both the coumarin and biphenyl scaffold. Antiproliferative studies against SKBr3 and MCF-7 breast cancer cell lines demonstrated these triazole-containing compounds to exhibit improved activity. These compounds were shown to manifest Hsp90 inhibitory activity through Western blot analysis and represent a new scaffold upon which more potent inhibitors can be pursued.

Original languageEnglish (US)
Pages (from-to)1317-1323
Number of pages7
Issue number9
StatePublished - Sep 2014
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry


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