Biological Activity of Water-Soluble Fullerenes. Structural Dependence of DNA Cleavage, Cytotoxicity, and Enzyme Inhibitory Activities Including HIV-Protease Inhibition

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Abstract

Two different classes of water-soluble fullerene derivatives, detergent-type and sphere-type, were synthesized. The derivatives were evaluated for their biological activities including cytotoxicity, DNA cleavage, and inhibition of HIV-protease and other enzymes. Both classes of compounds display generally similar behavior except for their cytotoxicity spectra against several cell lines. The fullerene derivatives bearing <i>N</i>-methylpyrrole were found to be photo-inactive with respect to DNA cleaving activity and cytotoxicity. A study on the kinetics for the inhibition of HIV-protease with detergent type derivative revealed that the compound is a potent fullerene-based HIV protease inhibitor, inhibiting the enzyme activity in a reversible and competitive manner with a <i>K</i><sub>i</sub> value of 0.32 μM.

Journal

  • Bulletin of the Chemical Society of Japan

    Bulletin of the Chemical Society of Japan 69(8), 2143-2151, 1996-08-15

    The Chemical Society of Japan

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Codes

  • NII Article ID (NAID)
    10008906738
  • NII NACSIS-CAT ID (NCID)
    AA00580132
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    00092673
  • NDL Article ID
    4060527
  • NDL Source Classification
    ZP1(科学技術--化学・化学工業)
  • NDL Call No.
    Z53-B35
  • Data Source
    CJP  CJPref  NDL  J-STAGE 
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