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Issue 9, 2014
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Triazole containing novobiocin and biphenyl amides as Hsp90 C-terminal inhibitors

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Abstract

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.

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

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Publication details

The article was received on 07 Mar 2014, accepted on 15 May 2014 and first published on 27 Jun 2014


Article type: Concise Article
DOI: 10.1039/C4MD00102H
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Citation: Med. Chem. Commun., 2014,5, 1317-1323

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

    J. Zhao, H. Zhao, J. A. Hall, D. Brown, E. Brandes, J. Bazzill, P. T. Grogan, C. Subramanian, G. Vielhauer, M. S. Cohen and B. S. J. Blagg, Med. Chem. Commun., 2014, 5, 1317
    DOI: 10.1039/C4MD00102H

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