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Triazole Containing Novobiocin and Biphenyl Amides as Hsp90 C-Terminal Inhibitors
dc.contributor.author | Zhao, Jinbo | |
dc.contributor.author | Zhao, Huiping | |
dc.contributor.author | Hall, Jessica Ann | |
dc.contributor.author | Brown, Douglas | |
dc.contributor.author | Brandes, Eileen | |
dc.contributor.author | Bazzill, Joseph | |
dc.contributor.author | Grogan, Patrick T. | |
dc.contributor.author | Subramanian, Chitra | |
dc.contributor.author | Vielhauer, George A. | |
dc.contributor.author | Cohen, Mark S. | |
dc.contributor.author | Blagg, Brian S. J. | |
dc.date.accessioned | 2017-06-22T17:15:36Z | |
dc.date.available | 2017-06-22T17:15:36Z | |
dc.date.issued | 2017-09-01 | |
dc.identifier.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 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/24575 | |
dc.description.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. | en_US |
dc.publisher | Royal Society of Chemistry | en_US |
dc.subject | Heat shock protein 90 | en_US |
dc.subject | Hsp90 C-terminal inhibitors | en_US |
dc.subject | Novobiocin | en_US |
dc.subject | Triazole | en_US |
dc.subject | Breast cancer | en_US |
dc.title | Triazole Containing Novobiocin and Biphenyl Amides as Hsp90 C-Terminal Inhibitors | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Zhao, Jinbo | |
kusw.kuauthor | Zhao, Huiping | |
kusw.kuauthor | Hall, Jessica A. | |
kusw.kuauthor | Blagg, Brian S. J. | |
kusw.kudepartment | Medicinal Chemistry | en_US |
dc.identifier.doi | 10.1039/C4MD00102H. | en_US |
dc.identifier.orcid | https://orcid.org/0000-0002-5261-7366 | |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.identifier.pmid | PMC4198308 | en_US |
dc.rights.accessrights | openAccess |