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Triazole Containing Novobiocin and Biphenyl Amides as Hsp90 C-Terminal Inhibitors
Zhao, Jinbo Zhao, Huiping Hall, Jessica Ann Brown, Douglas Brandes, Eileen Bazzill, Joseph Grogan, Patrick T. Subramanian, Chitra Vielhauer, George A. Cohen, Mark S.
Zhao, Jinbo
Zhao, Huiping
Hall, Jessica Ann
Brown, Douglas
Brandes, Eileen
Bazzill, Joseph
Grogan, Patrick T.
Subramanian, Chitra
Vielhauer, George A.
Cohen, Mark S.
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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.
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Date
2017-09-01
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Publisher
Royal Society of Chemistry
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Keywords
Heat shock protein 90, Hsp90 C-terminal inhibitors, Novobiocin, Triazole, Breast cancer
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