2-Phenylquinolones as inhibitors of the HIV-1 Tat-TAR interaction

ChemMedChem. 2009 Jun;4(6):935-8. doi: 10.1002/cmdc.200800437.

Abstract

Novel 2-phenylquinolones aimed at the Tat-TAR complex were synthesized and tested. Derivatives characterized by precise modifications of the quinolone nucleus and to the side chain of the 2-phenyl ring allowed a thorough structure-activity study, confirming 2-phenylquinolone as a suitable scaffold for inhibition of the Tat-TAR interaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / toxicity
  • Cell Line
  • HIV Long Terminal Repeat / drug effects*
  • HIV-1 / drug effects*
  • Humans
  • Jurkat Cells
  • Molecular Sequence Data
  • Protein Binding
  • Quinolones / chemical synthesis
  • Quinolones / chemistry*
  • Quinolones / toxicity
  • Structure-Activity Relationship
  • tat Gene Products, Human Immunodeficiency Virus / antagonists & inhibitors*
  • tat Gene Products, Human Immunodeficiency Virus / metabolism

Substances

  • Anti-HIV Agents
  • Quinolones
  • tat Gene Products, Human Immunodeficiency Virus