Optimization of anti-proliferative activity using a screening approachwith a series of bis-heterocyclic G-quadruplex ligands

Cristina Ciancimino, Mekala Gunaratnam, Stephen Neidle, Giulia Vignaroli, Cristina Ciancimino, Stephan A. Ohnmacht

Risultato della ricerca: Articlepeer review

14 Citazioni (Scopus)

Abstract

Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has beenidentified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The leadcompound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzeddirect arylation. The compound stabilizes several quadruplex DNA sequences including a human telomericDNA and one from the promoter of the HSP90 gene, although the structure–activity relationships of theseries are not obviously related to the quadruplex binding.
Lingua originaleEnglish
pagine (da-a)5351-5355
Numero di pagine5
RivistaBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume23
Stato di pubblicazionePublished - 2013

All Science Journal Classification (ASJC) codes

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

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