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dc.contributor.authorRossington, S.B.*
dc.contributor.authorHadfield, J.A.*
dc.contributor.authorShnyder, Steven D.*
dc.contributor.authorWallace, T.W.*
dc.contributor.authorWilliams, K.J.*
dc.date.accessioned2017-02-01T11:45:01Z
dc.date.available2017-02-01T11:45:01Z
dc.date.issued2017-03-01
dc.identifier.citationRossington SB, Hadfield JA, Shnyder SA et al (2017) Tubulin-binding dibenz[c,e]oxepines: Part 2. 1 Structural variation and biological evaluation as tumour vasculature disrupting agents. Bioorganic and Medicinal Chemistry. 25(5): 1630-1642.en_US
dc.identifier.urihttp://hdl.handle.net/10454/11235
dc.descriptionYesen_US
dc.description.abstract5,7-Dihydro-3,9,10,11-tetramethoxybenz[c,e]oxepin-4-ol 1, prepared from a dibenzyl ether precursor via Pd-catalysed intramolecular direct arylation, possesses broad-spectrum in vitro cytotoxicity towards various tumour cell lines, and induces vascular shutdown, necrosis and growth delay in tumour xenografts in mice at sub-toxic doses. The biological properties of 1 and related compounds can be attributed to their ability to inhibit microtubule assembly at the micromolar level, by binding reversibly to the same site of the tubulin αβ-heterodimer as colchicine 2 and the allocolchinol, N-acetylcolchinol 4.en_US
dc.language.isoenen_US
dc.relation.isreferencedbyhttp://dx.doi.org/10.1016/j.bmc.2017.01.027en_US
dc.rights© 2017 Elsevier. Reproduced in accordance with the publisher's selfarchiving policy. This manuscript version is made available under the CC-BY-NC-ND 4.0 license (http://creativecommons.org/licenses/by-nc-nd/4.0/)en_US
dc.subjectDibenz[c,e]oxepine; Iintramolecular direct arylation; Tubulin targeting; Tumour growth inhibition; Vascular shutdown; Colchicinoiden_US
dc.titleTubulin-binding dibenz[c,e]oxepines. Part 2. 1 Structural variation and biological evaluation as tumour vasculature disrupting agentsen_US
dc.status.refereedYesen_US
dc.date.Accepted2017-01-17
dc.date.application2017-01-19
dc.typeArticleen_US
dc.type.versionAccepted Manuscripten_US
refterms.dateFOA2018-01-20T00:00:00Z


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