Optimization of anti-proliferative activity using a screening approach with a series of bis-heterocyclic G-quadruplex ligands |
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Authors: | Stephan A Ohnmacht Cristina Ciancimino Giulia Vignaroli Mekala Gunaratnam Stephen Neidle |
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Institution: | UCL School of Pharmacy, University College London, WC1N 1AX London, UK |
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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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Keywords: | Quadruplex Anti-proliferative Phenotypic screening Telomerase Oxazoles |
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