Synthesis and biological evaluation of novel 4,5-bis(dialkylaminoalkyl)-substituted acridines as potent telomeric G-quadruplex ligands

Eur J Med Chem. 2009 Oct;44(10):3880-8. doi: 10.1016/j.ejmech.2009.04.021. Epub 2009 Apr 22.

Abstract

Several 4,5-bis(dialkylaminoalkyl)-substituted acridines have been prepared starting from acridine and their telomeric G-quadruplex stabilizing properties were evaluated using FRET melting and TRAP (Telomerase Repeat Amplification Protocol Assay) experiments.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acridines / chemical synthesis
  • Acridines / chemistry*
  • Acridines / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Fluorescence Resonance Energy Transfer
  • G-Quadruplexes / drug effects*
  • Humans
  • Ligands
  • Molecular Structure
  • Nucleic Acid Denaturation / drug effects
  • Telomerase / antagonists & inhibitors
  • Telomerase / metabolism
  • Telomere / drug effects*

Substances

  • Acridines
  • Antineoplastic Agents
  • Ligands
  • Telomerase