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    Cross-linking and sequence specific alkylation of DNA by aziridinyl quinones. 2. Structure requirements for sequence selectivity.

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    Authors
    Hargreaves, Robert H J
    Mayalarp, Stephen P
    Butler, John
    McAdam, S R
    O'Hare, C C
    Hartley, John A
    Affiliation
    CRC Department of Biophysical Chemistry, Drug Development, Paterson Institute for Cancer Research, Christie Hospital NHS Trust, Manchester, U.K.
    Issue Date
    1997-01-31
    
    Metadata
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    Abstract
    The cytotoxicities and DNA sequence selectivity for guanine-N7 alkylation of 22 mono- and disubstituted 2,5-diaziridinyl-1,4-benzoquinones have been investigated. Several quinones produced patterns of alkylation following reduction with a selectivity for 5'-TGC-3' sequences. This sequence selectivity appeared to be dependent only on the presence of a hydrogen in position-6 of the quinone. A computer model, based on published crystallographic data, was used to explain this selectivity. The sequence selective quinones were generally more cytotoxic that the quinones which reacted randomly.
    Citation
    Cross-linking and sequence specific alkylation of DNA by aziridinyl quinones. 2. Structure requirements for sequence selectivity. 1997, 40 (3):357-61 J. Med. Chem.
    Journal
    Journal of Medicinal Chemistry
    URI
    http://hdl.handle.net/10541/95491
    DOI
    10.1021/jm960492j
    PubMed ID
    9022802
    Type
    Article
    Language
    en
    ISSN
    0022-2623
    ae974a485f413a2113503eed53cd6c53
    10.1021/jm960492j
    Scopus Count
    Collections
    All Paterson Institute for Cancer Research

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