Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has been identified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The lead compound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzed direct arylation. The compound stabilizes several quadruplex DNA sequences including a human telomeric DNA and one from the promoter of the HSP90 gene, although the structure–activity relationships of the series are not obviously related to the quadruplex binding.
Ohnmacht, S.A., Ciancimino, C., Vignaroli, G., Gunaratnam, M., Neidle, S. (2013). Optimization of anti-proliferative activity using a screening approach with a series of bis-heterocyclic G-quadruplex ligands. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 23(23), 5351-5355 [http://dx.doi.org/10.1016/j.bmcl.2013.07.057].
Optimization of anti-proliferative activity using a screening approach with a series of bis-heterocyclic G-quadruplex ligands
CIANCIMINO, Cristina;
2013-01-01
Abstract
Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has been identified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The lead compound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzed direct arylation. The compound stabilizes several quadruplex DNA sequences including a human telomeric DNA and one from the promoter of the HSP90 gene, although the structure–activity relationships of the series are not obviously related to the quadruplex binding.
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