Design, Synthesis and Biological Evaluation of Biphenylamide Derivatives as Hsp90 C-terminal Inhibitors
dc.contributor.author | Zhao, Huiping | |
dc.contributor.author | Garg, Gaurav | |
dc.contributor.author | Zhao, Jinbo | |
dc.contributor.author | Moroni, Elisabetta | |
dc.contributor.author | Girgis, Antwan | |
dc.contributor.author | Franco, Lucas S. | |
dc.contributor.author | Singh, Swapnil | |
dc.contributor.author | Colombo, Giorgio | |
dc.contributor.author | Blagg, Brian S. J. | |
dc.date.accessioned | 2017-06-12T17:16:42Z | |
dc.date.available | 2017-06-12T17:16:42Z | |
dc.date.issued | 2015-01-07 | |
dc.identifier.citation | Zhao, H., Garg, G., Zhao, J., Moroni, E., Girgis, A., Franco, L. S., … Blagg, B. S. J. (2015). Design, Synthesis and Biological Evaluation of Biphenylamide Derivatives as Hsp90 C-terminal Inhibitors. European Journal of Medicinal Chemistry, 89, 442–466. http://doi.org/10.1016/j.ejmech.2014.10.034 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/24468 | |
dc.description.abstract | Modulation of Hsp90 C-terminal function represents a promising therapeutic approach for the treatment of cancer and neurodegenerative diseases. Current drug discovery efforts toward Hsp90 C-terminal inhibition focus on novobiocin, an antibiotic that was transformed into an Hsp90 inhibitor. Based on structural information obtained during the development of novobiocin derivatives and molecular docking studies, scaffolds containing a biphenyl moiety in lieu of the coumarin ring present in novobiocin were identified as new Hsp90 C-terminal inhibitors. Structure-activity relationship studies produced new derivatives that inhibit the proliferation of breast cancer cell lines at nanomolar concentrations, which corresponded directly with Hsp90 inhibition. | en_US |
dc.publisher | Elsevier | en_US |
dc.rights | This is an open access article under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs License 4.0 (CC BY-NC-ND 4.0), which permits use and distribution in any medium, provided the original work is properly cited, the use is non-commercial and no modifications or adaptations are made. | en_US |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | en_US |
dc.subject | Heat shock protein 90 | en_US |
dc.subject | Hsp90 C-terminal inhibitors | en_US |
dc.subject | Biphenyl | en_US |
dc.subject | Structure-activity relationship | en_US |
dc.subject | Breast cancer | en_US |
dc.title | Design, Synthesis and Biological Evaluation of Biphenylamide Derivatives as Hsp90 C-terminal Inhibitors | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Zhao, Huiping | |
kusw.kuauthor | Garg, Gaurav | |
kusw.kuauthor | Zhao, Jinbo | |
kusw.kuauthor | Girgis, Antwan | |
kusw.kuauthor | Franco, Lucas S. | |
kusw.kuauthor | Singh, Swapnil | |
kusw.kuauthor | Blagg, Brian S. J. | |
kusw.kudepartment | Medicinal Chemistry | en_US |
dc.identifier.doi | 10.1016/j.ejmech.2014.10.034 | 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 | PMC4406240 | en_US |
dc.rights.accessrights | openAccess |
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Except where otherwise noted, this item's license is described as: This is an open access article under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs License 4.0 (CC BY-NC-ND 4.0), which permits use and distribution in any medium, provided the original work is properly cited, the use is non-commercial and no modifications or adaptations are made.