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    Towards more specific O6-methylguanine-DNA methyltransferase (MGMT) inactivators.

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    Authors
    Lopez, S
    Margison, Geoffrey P
    McElhinney, R
    Cordeiro, A
    McMurry, T
    Rozas, I
    Affiliation
    School of Chemistry, University of Dublin, Trinity College, Dublin 2, Ireland.
    Issue Date
    2011-03-01
    
    Metadata
    Show full item record
    Abstract
    Searching for a novel family of inactivators of the human DNA repair protein O(6)-methylguanine-DNA methyltransferase (MGMT) which is known to bind to the DNA minor groove, we have computationally modelled and synthesised two series of 2-amino-6-aryloxy-5-nitropyrimidines with morpholino or aminodiaryl substituents (potential minor groove binders) at the 4-position. Synthesis of these compounds was achieved by successive substitution of each of the two Cl atoms of 2-amino-4,6-dichloro-5-nitropyrimidine by the corresponding amino and aryloxy derivatives. Biochemical evaluation of these compounds as MGMT inactivators showed poor activities, but in general the 4-bromothenyloxy derivatives showed better inactivation than the benzyloxy versions. DNA binding assessment was not possible due to insolubility problems.
    Citation
    Towards more specific O6-methylguanine-DNA methyltransferase (MGMT) inactivators. 2011, 19 (5):1658-65 Bioorg Med Chem
    Journal
    Bioorganic & Medicinal Chemistry
    URI
    http://hdl.handle.net/10541/192872
    DOI
    10.1016/j.bmc.2011.01.038
    PubMed ID
    21320783
    Type
    Article
    Language
    en
    ISSN
    1464-3391
    ae974a485f413a2113503eed53cd6c53
    10.1016/j.bmc.2011.01.038
    Scopus Count
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    All Paterson Institute for Cancer Research

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