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Novobiocin analogues with second-generation noviose surrogates

dc.contributor.authorZhao, Huiping
dc.contributor.authorBlagg, Brian S. J.
dc.date.accessioned2017-05-04T18:04:41Z
dc.date.available2017-05-04T18:04:41Z
dc.date.issued2013-01-15
dc.identifier.citationZhao, H., & Blagg, B. S. J. (2013). Novobiocin analogues with second-generation noviose surrogates. Bioorganic & Medicinal Chemistry Letters, 23(2), 552–557. http://doi.org/10.1016/j.bmcl.2012.11.022en_US
dc.identifier.urihttp://hdl.handle.net/1808/23891
dc.description.abstractHsp90 is a promising therapeutic target for the treatment of cancer. Novobiocin is the first Hsp90 C-terminal inhibitor ever identified and recent structure-activity relationship studies on the noviose sugar identified several commercially available amines as suitable surrogates. In an effort to further understand this region of the molecule, analogues containing various N′-amino substituents were prepared and evaluated against two breast cancer cell lines for determination of their efficacy. Compound 37j manifested the most potent anti-proliferative activity from these studies and induced Hsp90-dependent client protein degradation at mid nano-molar concentrations.en_US
dc.publisherElsevieren_US
dc.rightsThis article is made available under an Attribution-NonCommercial-NoDerivs 3.0 United States (CC BY-NC-ND 3.0 US) License.en_US
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/3.0/us/en_US
dc.subjectHeat shock protein 90en_US
dc.subjectHsp90 inhibitorsen_US
dc.subjectNovobiocin analoguesen_US
dc.subjectBreast canceren_US
dc.titleNovobiocin analogues with second-generation noviose surrogatesen_US
dc.typeArticleen_US
kusw.kuauthorZhao, Huiping
kusw.kuauthorBlagg, Brian S. J.
kusw.kudepartmentMedicinal Chemistryen_US
dc.identifier.doi10.1016/j.bmcl.2012.11.022en_US
kusw.oaversionScholarly/refereed, author accepted manuscripten_US
kusw.oapolicyThis item meets KU Open Access policy criteria.en_US
dc.identifier.pmidPMC4123793en_US
dc.rights.accessrightsopenAccess


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