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dc.contributor.authorDi Francesco, A
dc.contributor.authorHargreaves, R
dc.contributor.authorWallace, T
dc.contributor.authorMayalarp, Stephen P
dc.contributor.authorHazrati, A
dc.contributor.authorHartley, J
dc.contributor.authorButler, John
dc.date.accessioned2010-01-20T14:53:15Z
dc.date.available2010-01-20T14:53:15Z
dc.date.issued2000-10
dc.identifier.citationThe abnormal cytotoxicities of 2,5-diaziridinyl-1,4-benzoquinone-3-phenyl esters. 2000, 15 (5):347-59 Anticancer Drug Des.en
dc.identifier.issn0266-9536
dc.identifier.pmid11354311
dc.identifier.urihttp://hdl.handle.net/10541/90129
dc.description.abstractSeveral derivatives of 2,5-diaziridinyl-3-phenyl-1,4-benzoquinone have been synthesized and their cytotoxicities in six different human cancer cell lines (H460, H596, HT29, BE, K562 and A2780) have been determined. It was observed that certain phenol-ester derivatives were significantly more cytotoxic in all of the cell lines investigated. These esters were shown to be cleaved by esterases to form a stable meta-phenol and an unstable para-phenol. The meta-phenol was also highly cytotoxic. Several of these compounds were studied in detail using DNA cross-linking, clonogenic, apoptosis and flow cytometry assays. It is proposed that although the phenol-esters and the phenols can efficiently cross-link DNA, this mechanism alone is not sufficient to explain the toxicities of these compounds.
dc.language.isoenen
dc.subjectCultured Tumour Cellsen
dc.subject.meshAntineoplastic Agents
dc.subject.meshApoptosis
dc.subject.meshBenzoquinones
dc.subject.meshCell Cycle
dc.subject.meshCell Survival
dc.subject.meshChromatography, High Pressure Liquid
dc.subject.meshClone Cells
dc.subject.meshCross-Linking Reagents
dc.subject.meshElectrophoresis
dc.subject.meshEsterases
dc.subject.meshEsters
dc.subject.meshFlow Cytometry
dc.subject.meshHumans
dc.subject.meshIndicators and Reagents
dc.subject.meshMolecular Conformation
dc.subject.meshNAD(P)H Dehydrogenase (Quinone)
dc.subject.meshStereoisomerism
dc.subject.meshStructure-Activity Relationship
dc.subject.meshTumor Cells, Cultured
dc.titleThe abnormal cytotoxicities of 2,5-diaziridinyl-1,4-benzoquinone-3-phenyl esters.en
dc.typeArticleen
dc.contributor.departmentDepartment of Biological Sciences, Salford University, UK.en
dc.identifier.journalAnti-Cancer Drug Designen
html.description.abstractSeveral derivatives of 2,5-diaziridinyl-3-phenyl-1,4-benzoquinone have been synthesized and their cytotoxicities in six different human cancer cell lines (H460, H596, HT29, BE, K562 and A2780) have been determined. It was observed that certain phenol-ester derivatives were significantly more cytotoxic in all of the cell lines investigated. These esters were shown to be cleaved by esterases to form a stable meta-phenol and an unstable para-phenol. The meta-phenol was also highly cytotoxic. Several of these compounds were studied in detail using DNA cross-linking, clonogenic, apoptosis and flow cytometry assays. It is proposed that although the phenol-esters and the phenols can efficiently cross-link DNA, this mechanism alone is not sufficient to explain the toxicities of these compounds.


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