Triazole Containing Novobiocin and Biphenyl Amides as Hsp90 C-Terminal Inhibitors
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Issue Date
2017-09-01Author
Zhao, Jinbo
Zhao, Huiping
Hall, Jessica Ann
Brown, Douglas
Brandes, Eileen
Bazzill, Joseph
Grogan, Patrick T.
Subramanian, Chitra
Vielhauer, George A.
Cohen, Mark S.
Blagg, Brian S. J.
Publisher
Royal Society of Chemistry
Type
Article
Article Version
Scholarly/refereed, author accepted manuscript
Metadata
Show full item recordAbstract
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.
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Citation
Zhao, J., Zhao, H., Hall, J. A., Brown, D., Brandes, E., Bazzill, J., … Blagg, B. S. J. (2014). Triazole Containing Novobiocin and Biphenyl Amides as Hsp90 C-Terminal Inhibitors. MedChemComm, 5(9), 1317–1323. http://doi.org/10.1039/C4MD00102H
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