ATTENTION: The software behind KU ScholarWorks is being upgraded to a new version. Starting July 15th, users will not be able to log in to the system, add items, nor make any changes until the new version is in place at the end of July. Searching for articles and opening files will continue to work while the system is being updated.
If you have any questions, please contact Marianne Reed at mreed@ku.edu .
Engineering an Antibiotic to Fight Cancer: Optimization of the Novobiocin Scaffold to Produce Anti-Proliferative Agents
dc.contributor.author | Zhao, Huiping | |
dc.contributor.author | Donnelly, Alison C. | |
dc.contributor.author | Kusuma, Bhaskar Reddy | |
dc.contributor.author | Brandt, Gary E. L. | |
dc.contributor.author | Brown, Douglas | |
dc.contributor.author | Rajewski, Roger A. | |
dc.contributor.author | Bielhauer, George | |
dc.contributor.author | Holzbeierlein, Jeffery M. | |
dc.contributor.author | Cohen, Mark S. | |
dc.contributor.author | Blagg, Brian S. J. | |
dc.date.accessioned | 2017-04-06T16:58:07Z | |
dc.date.available | 2017-04-06T16:58:07Z | |
dc.date.issued | 2011-06-09 | |
dc.identifier.citation | Zhao, H., Donnelly, A. C., Kusuma, B. R., Brandt, G. E. L., Brown, D., Rajewski, R. A., … Blagg, B. S. J. (2011). Engineering an Antibiotic to Fight Cancer: Optimization of the Novobiocin Scaffold to Produce Anti-Proliferative Agents. Journal of Medicinal Chemistry, 54(11), 3839–3853. http://doi.org/10.1021/jm200148p | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/23591 | |
dc.description.abstract | Development of the DNA gyrase inhibitor, novobiocin, into a selective Hsp90 inhibitor was accomplished through structural modifications to the amide side chain, coumarin ring, and sugar moiety. These species exhibit ~700-fold improved anti-proliferative activity versus the natural product as evaluated by cellular efficacies against breast, colon, prostate, lung, and other cancer cell lines. Utilization of structure–activity relationships established for three novobiocin synthons produced optimized scaffolds, which manifest mid-nanomolar activity against a panel of cancer cell lines and serve as lead compounds that manifest their activities through Hsp90 inhibition. | en_US |
dc.publisher | American Chemical Society | en_US |
dc.rights | This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/jm200148p. | en_US |
dc.title | Engineering an Antibiotic to Fight Cancer: Optimization of the Novobiocin Scaffold to Produce Anti-Proliferative Agents | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Zhao, Huiping | |
kusw.kuauthor | Donnelly, Alison C. | |
kusw.kuauthor | Kusuma, Bhaskar Reddy | |
kusw.kuauthor | Brandt, Gary E. L. | |
kusw.kuauthor | Brown, Douglas | |
kusw.kuauthor | Rajewski, Roger A. | |
kusw.kuauthor | Vielhaur, George | |
kusw.kuauthor | Holzbeirerlein, Jeffrey | |
kusw.kuauthor | Cohen, Mark S. | |
kusw.kuauthor | Blagg, Brian S. J. | |
dc.identifier.doi | 10.1021/jm200148p | en_US |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.rights.accessrights | openAccess |