The abnormal cytotoxicities of 2,5-diaziridinyl-1,4-benzoquinone-3-phenyl esters.

2.50
Hdl Handle:
http://hdl.handle.net/10541/90129
Title:
The abnormal cytotoxicities of 2,5-diaziridinyl-1,4-benzoquinone-3-phenyl esters.
Authors:
Di Francesco, A; Hargreaves, R; Wallace, T; Mayalarp, Stephen P; Hazrati, A; Hartley, J; Butler, John
Abstract:
Several 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.
Affiliation:
Department of Biological Sciences, Salford University, UK.
Citation:
The abnormal cytotoxicities of 2,5-diaziridinyl-1,4-benzoquinone-3-phenyl esters. 2000, 15 (5):347-59 Anticancer Drug Des.
Journal:
Anti-Cancer Drug Design
Issue Date:
Oct-2000
URI:
http://hdl.handle.net/10541/90129
PubMed ID:
11354311
Type:
Article
Language:
en
ISSN:
0266-9536
Appears in Collections:
All Paterson Institute for Cancer Research

Full metadata record

DC FieldValue Language
dc.contributor.authorDi Francesco, Aen
dc.contributor.authorHargreaves, Ren
dc.contributor.authorWallace, Ten
dc.contributor.authorMayalarp, Stephen Pen
dc.contributor.authorHazrati, Aen
dc.contributor.authorHartley, Jen
dc.contributor.authorButler, Johnen
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.en
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
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