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

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    Authors
    Di Francesco, A
    Hargreaves, R
    Wallace, T
    Mayalarp, Stephen P
    Hazrati, A
    Hartley, J
    Butler, John
    Affiliation
    Department of Biological Sciences, Salford University, UK.
    Issue Date
    2000-10
    
    Metadata
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    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.
    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
    URI
    http://hdl.handle.net/10541/90129
    PubMed ID
    11354311
    Type
    Article
    Language
    en
    ISSN
    0266-9536
    Collections
    All Paterson Institute for Cancer Research

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