Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands.

F. Cuenca, O. Greciano, M. Gunaratnam, Shozeb Haider, D. Munnur, R. Nanjunda, W.D. Wilson, S. Neidle

Research output: Contribution to journalArticlepeer-review

106 Citations (Scopus)


A series of tri- and tetra-substituted naphthalene diimides have been designed and synthesized. Several compounds show exceptional affinity for telomeric G-quadruplex DNA in classical and competition FRET assays and SPR studies. They inhibit telomerase in the TRAP assay, and show potent senescence-based short-term anti-proliferative effects on MCF7 and A549 cancer cell lines, and localize in the nucleus and particularly the nucleolus of MCF7 cells.
Original languageEnglish
Pages (from-to)1668-1673
Number of pages6
JournalBioorganic & Medicinal Chemistry Letters
Issue number5
Publication statusPublished - 01 Mar 2008

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science


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