Inhibition of HIV-1 nuclear import via schiff base formation with arylene bis(methylketone) compounds

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3117-9. doi: 10.1016/s0960-894x(02)00642-x.

Abstract

Arylene bis(methylketone) compounds specifically block nuclear translocation of the HIV-1 pre-integration complex by forming Schiff-base adducts with contiguous lysines within nuclear localization signal.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Active Transport, Cell Nucleus / drug effects*
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Cell Nucleus / chemistry
  • Cell Nucleus / drug effects
  • Cell Nucleus / virology*
  • Cells, Cultured
  • HIV-1 / drug effects*
  • Humans
  • Indicators and Reagents
  • Ketones / chemical synthesis*
  • Ketones / pharmacology*
  • Macrophages / drug effects
  • Macrophages / ultrastructure
  • Macrophages / virology
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology*
  • Reverse Transcriptase Polymerase Chain Reaction
  • Schiff Bases / chemistry*
  • Structure-Activity Relationship

Substances

  • Anti-HIV Agents
  • Indicators and Reagents
  • Ketones
  • Pyrimidines
  • Schiff Bases