Di Francesco, AM; Hargreaves, RHJ; Wallace, TW; Mayalarp, SP; Hazratis, A; Hartley, JA; Butler, J; (2000) The abnormal cytotoxicities of 2,5-diaziridinyl-1,4-benzoquinone-3-phenyl esters. ANTI-CANCER DRUG DES , 15 (5) 347 - 359.
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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.
|Title:||The abnormal cytotoxicities of 2,5-diaziridinyl-1,4-benzoquinone-3-phenyl esters|
|Keywords:||diaziridinylquinones, ester isomers, DT-diaphorase, DNA crosslinking, OXIDOREDUCTASE DT-DIAPHORASE, SEQUENCE-SPECIFIC ALKYLATION, CROSS-LINKING, COMET ASSAY, ADENOCARCINOMA CELLS, ANTITUMOR QUINONES, DNA, DIAZIRIDINYLBENZOQUINONES, BENZOQUINONES, AZIRIDINYLQUINONES|
|UCL classification:||UCL > School of Life and Medical Sciences > Faculty of Medical Sciences > Wolfson Institute and Cancer Institute Administration > Cancer Institute > Research Department of Oncology|
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