dc.contributor.author | Kusuma, Bhaskar Reddy | |
dc.contributor.author | Khandelwal, Anuj | |
dc.contributor.author | Gu, Wen | |
dc.contributor.author | Brown, Douglas | |
dc.contributor.author | Liu, Weiya | |
dc.contributor.author | Vielhauer, George A. | |
dc.contributor.author | Holzbeierlein, Jeffery M. | |
dc.contributor.author | Blagg, Brian S. J. | |
dc.date.accessioned | 2017-05-10T18:40:01Z | |
dc.date.available | 2017-05-10T18:40:01Z | |
dc.date.issued | 2014-02-15 | |
dc.identifier.citation | Kusuma, B. R., Khandelwal, A., Gu, W., Brown, D., Liu, W., Vielhauer, G., … Blagg, B. S. J. (2014). Synthesis and Biological Evaluation of Coumarin Replacements of Novobiocin as Hsp90 Inhibitors. Bioorganic & Medicinal Chemistry, 22(4), 1441–1449. http://doi.org/10.1016/j.bmc.2013.12.056 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/24082 | |
dc.description.abstract | Since Hsp90 modulates all six hallmarks of cancer simultaneously, it has become an attractive target for the development of cancer chemotherapeutics. In an effort to develop more efficacious compounds for Hsp90 inhibition, novobiocin analogues were prepared by replacing the central coumarin core with naphthalene, quinolinone, and quinoline surrogates. These modifications allowed for modification of the 2-position, which was previously unexplored. Biological evaluation of these compounds suggests a hydrophobic pocket about the 2-position of novobiocin. Anti-proliferative activities of these analogues against multiple cancer cell lines identified 2-alkoxyquinoline derivatives to exhibit improved activity. | en_US |
dc.publisher | Elsevier | en_US |
dc.rights | This article is made available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0)
License. | en_US |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/3.0/ | en_US |
dc.title | Synthesis and Biological Evaluation of Coumarin Replacements of Novobiocin as Hsp90 Inhibitors | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Kusuma, Bhaskar Reddy | |
kusw.kuauthor | Khandelwal, Anuj | |
kusw.kuauthor | Gu, Wen | |
kusw.kuauthor | Blagg, Brian S. J. | |
kusw.kudepartment | Medicinal Chemistry | en_US |
kusw.oanotes | Per SherpaRomeo on 05/10/2017: Author's Pre-print: green tick author can archive pre-print (ie pre-refereeing) Author's Post-print: green tick author can archive post-print (ie final draft post-refereeing) Publisher's Version/PDF: cross author cannot archive publisher's version/PDF General Conditions: Authors pre-print on any website, including arXiv and RePEC Author's post-print on author's personal website immediately Author's post-print on open access repository after an embargo period of between 12 months and 48 months Permitted deposit due to Funding Body, Institutional and Governmental policy or mandate, may be required to comply with embargo periods of 12 months to 48 months Author's post-print may be used to update arXiv and RepEC Publisher's version/PDF cannot be used Must link to publisher version with DOI Author's post-print must be released with a Creative Commons Attribution Non-Commercial No Derivatives License | en_US |
dc.identifier.doi | 10.1016/j.bmc.2013.12.056 | en_US |
dc.identifier.orcid | https://orcid.org/0000-0003-4492-4400 | |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.identifier.pmid | PMC3963410 | en_US |
dc.rights.accessrights | openAccess | |