| dc.contributor.author | Kusuma, Bhaskar Reddy | |
| dc.contributor.author | Peterson, Laura B. | |
| dc.contributor.author | Zhao, Huiping | |
| dc.contributor.author | Vielhauer, George A. | |
| dc.contributor.author | Holzbeierlein, Jeffery M. | |
| dc.contributor.author | Blagg, Brian S. J. | |
| dc.date.accessioned | 2017-04-12T16:15:35Z | |
| dc.date.available | 2017-04-12T16:15:35Z | |
| dc.date.issued | 2011-09-22 | |
| dc.identifier.citation | Kusuma, B. R., Peterson, L. B., Zhao, H., Vielhauer, G., Holzbeierlein, J., & Blagg, B. S. J. (2011). Targeting the Heat Shock Protein 90 Dimer with Dimeric Inhibitors. Journal of Medicinal Chemistry, 54(18), 6234–6253. http://doi.org/10.1021/jm200553w | en_US |
| dc.identifier.uri | http://hdl.handle.net/1808/23632 | |
| dc.description.abstract | The design, synthesis and biological evaluation of conformationally constrained coumermycin A1 analogues are reported. Compounds were evaluated against both breast cancer (SKBr3 and MCF7) and prostate cancer (PC3mm2, A549 and HT29) cell lines. Non-noviosylated coumermycin A1 analogues that manifest potent anti-proliferative activity resulting from Hsp90 inhibition are provided, wherein replacement of the stereochemically complex noviose sugar with readily available piperidine rings resulted in ~100 fold increase in anti-proliferative activities as compared to coumermycin A1, producing small molecule Hsp90 inhibitors that exhibit nanomolar activities. | 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/jm200553w. | en_US |
| dc.title | Targeting the Heat Shock Protein 90 Dimer with Dimeric Inhibitors | en_US |
| dc.type | Article | en_US |
| kusw.kuauthor | Kusuma, Bhaskar Reddy | |
| kusw.kuauthor | Peterson, Laura B. | |
| kusw.kuauthor | Zhao, Huiping | |
| kusw.kuauthor | Vielhauer, George | |
| kusw.kuauthor | Holzbeierlein, Jeffrey | |
| kusw.kuauthor | Blagg, Brian S. J. | |
| kusw.kudepartment | Medicinal Chemistry | en_US |
| dc.identifier.doi | 10.1021/jm200553w | 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 | |
