A Novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines

Caterina M. Lombardo, Sarah J. Welsh, Sandra J. Strauss, Aaron G. Dale, Alan K. Todd, Rupesh Nanjunda, W. David Wilson, Stephen Neidle

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

A series of naphthalene derivatives with disubstituted triazole side-arms have been assembled by click chemistry. Lead compounds show a high level of selectivity for renal, osteo- and Ewing's sarcomas that express the HIF-1∝ transcription factor. They also interact selectively with the quadruplex DNAs located in the promoter of the HIF genes and it is suggested that the mechanism of action involves inhibition of transcription by drug-mediated quadruplex stabilization in these regions.
Original languageEnglish
Pages (from-to)5984-5988
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number18
DOIs
Publication statusPublished - 2012
Externally publishedYes

Keywords

  • HIF
  • Quadruplex
  • Renal cancer
  • Sarcomas
  • Small molecule

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