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Synthesis and Biological Evaluation of Coumarin Replacements of Novobiocin as Hsp90 Inhibitors

dc.contributor.authorKusuma, Bhaskar Reddy
dc.contributor.authorKhandelwal, Anuj
dc.contributor.authorGu, Wen
dc.contributor.authorBrown, Douglas
dc.contributor.authorLiu, Weiya
dc.contributor.authorVielhauer, George A.
dc.contributor.authorHolzbeierlein, Jeffery M.
dc.contributor.authorBlagg, Brian S. J.
dc.date.accessioned2017-05-10T18:40:01Z
dc.date.available2017-05-10T18:40:01Z
dc.date.issued2014-02-15
dc.identifier.citationKusuma, 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.2013.12.056en_US
dc.identifier.urihttp://hdl.handle.net/1808/24082
dc.description.abstractSince 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.publisherElsevieren_US
dc.rightsThis 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.urihttps://creativecommons.org/licenses/by-nc-nd/3.0/en_US
dc.titleSynthesis and Biological Evaluation of Coumarin Replacements of Novobiocin as Hsp90 Inhibitorsen_US
dc.typeArticleen_US
kusw.kuauthorKusuma, Bhaskar Reddy
kusw.kuauthorKhandelwal, Anuj
kusw.kuauthorGu, Wen
kusw.kuauthorBlagg, Brian S. J.
kusw.kudepartmentMedicinal Chemistryen_US
kusw.oanotesPer 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 Licenseen_US
dc.identifier.doi10.1016/j.bmc.2013.12.056en_US
dc.identifier.orcidhttps://orcid.org/0000-0003-4492-4400
kusw.oaversionScholarly/refereed, author accepted manuscripten_US
kusw.oapolicyThis item meets KU Open Access policy criteria.en_US
dc.identifier.pmidPMC3963410en_US
dc.rights.accessrightsopenAccess


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This article is made available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License.
Except where otherwise noted, this item's license is described as: This article is made available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License.