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dc.contributor.authorPors, Klaus*
dc.contributor.authorCasely-Hayford, M.A.*
dc.contributor.authorHartley, J.A.*
dc.contributor.authorPatterson, Laurence H.*
dc.contributor.authorSearcey, M.*
dc.date.accessioned2009-12-16T09:38:17Z
dc.date.available2009-12-16T09:38:17Z
dc.date.issued2005
dc.identifier.citationPors, K., Casely-Hayford, M., Hartley, J.A. and Patterson, L.H. (2005). Design and synthesis of a DNA-crosslinking azinomycin analogue. Organic & Biomolecular Chemistry. Vol. 3, No. 19, pp. 3585-3589.
dc.identifier.urihttp://hdl.handle.net/10454/4115
dc.descriptionNo
dc.description.abstractThe azinomycins are potent antitumour antibiotics that are able to crosslink DNA, but are relatively unstable and unlikely to progress as therapeutic candidates. A prototype analogue 4 with more clinical potential has been designed and synthesised and incorporates the epoxide function of the azinomycins and a nitrogen mustard. Two further analogues 5 and 6 that can alkylate DNA but cannot crosslink the duplex have also been synthesised. Compound 4 crosslinks DNA efficiently at nM concentrations. Compounds 4¿6 were submitted to the NCI 60 cell line screen and have similar antitumour activity, although 4 is slightly less active than the non-crosslinking compounds. These observations will be important in the design of further azinomycin analogues with antitumour activity.
dc.language.isoen
dc.subjectDNA-crosslinking
dc.subjectAzinomycin Analogue
dc.subjectCancer Therapeutics
dc.titleDesign and synthesis of a DNA-crosslinking azinomycin analogue
dc.status.refereedYes
dc.typeArticle
dc.type.versionNo full-text in the repository
dc.identifier.doihttps://doi.org/10.1039/b508908e
dc.openaccess.statusclosedAccess


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