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.
|Numero di pagine||5|
|Rivista||BIOORGANIC & MEDICINAL CHEMISTRY LETTERS|
|Stato di pubblicazione||Published - 2013|
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