Synthesis and biological evaluation of novel isoellipticine derivatives and salts

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dc.contributor.authorMiller, Charlotte M.
dc.contributor.authorO’Sullivan, Elaine C.
dc.contributor.authorDevine, Ken J.
dc.contributor.authorMcCarthy, Florence O.
dc.contributor.funderHigher Education Authority
dc.date.accessioned2024-02-20T12:48:03Z
dc.date.available2024-02-19T17:10:44Zen
dc.date.available2024-02-20T12:48:03Z
dc.date.issued2012-08-24
dc.date.updated2024-02-19T17:10:46Zen
dc.description.abstractSynthesis of novel 7-substituted isoellipticines and isoellipticinium salts is described, with optimisation of routes, representing a new class of anti-cancer agent. Initial assessment of biological activity using a topoisomerase II decatenation assay and NCI screening highlighted strong anti-cancer activity, further developed in a panel of isoellipticinium salts. Interestingly, low correlation between results of the topoisomerase II decatenation assay and NCI screen throughout the panel suggest that topo II is not the most important biological target with respect to anti-cancer activity in this new class of compounds. Results also suggest that solubility is not the limiting factor in activity of the isoellipticinium salts. Overall, 20 novel ellipticine analogues were prepared and full anti-cancer profiling was completed for 13 isoellipticine derivatives and salts. Two compounds display significant specificity towards CNS cancer cell lines and are lead compounds for future development.en
dc.description.sponsorshipHigher Education Authority (PRTLI4)
dc.description.statusPeer revieweden
dc.description.versionAccepted Version
dc.format.mimetypeapplication/pdfen
dc.identifier.citationMiller, C. M., O'Sullivan, E. C., Devine, K. J. and McCarthy, F. O. (2012) 'Synthesis and biological evaluation of novel isoellipticine derivatives and salts', Organic and Biomolecular Chemistry, 10(39), pp. 7912-7921. doi: https://doi.org/10.1039/C2OB26181B
dc.identifier.doihttps://doi.org/10.1039/C2OB26181B
dc.identifier.eissn1477-0539
dc.identifier.endpage7921
dc.identifier.issn1477-0520
dc.identifier.issued39
dc.identifier.journaltitleOrganic and Biomolecular Chemistry
dc.identifier.startpage7912
dc.identifier.urihttps://hdl.handle.net/10468/15566
dc.identifier.volume10
dc.language.isoenen
dc.publisherRoyal Society of Chemistry
dc.rights© 2012, The Royal Society of Chemistry. All rights reserved.
dc.subjectIsoellipticine
dc.subjectEllipticine
dc.subjectCancer
dc.subjectTopoisomerase
dc.titleSynthesis and biological evaluation of novel isoellipticine derivatives and salts
dc.typeArticle (peer-reviewed)
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