Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 10, Issue 32, Pages 6537-6546Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob25830g
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Funding
- Cancer Research UK
- MUIR FIRB-Ideas [RBID082ATK]
- Ligue Nationale Contre le Cancer
- BBSRC [BB/G008337/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/G008337/1] Funding Source: researchfish
- Cancer Research UK [11961, 12488] Funding Source: researchfish
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The synthesis, biophysical and biological evaluation of a series of G-quadruplex interacting small molecules based on a N,N'-bis(quinolinyl) pyridine-2,6-dicarboxamide scaffold is described. The synthetic analogues were evaluated for their ability to stabilize telomeric G-quadruplex DNA, some of which showed very high stabilization potential associated with high selectivity over double-stranded DNA. The compounds exhibited growth arrest of cancer cells with detectable selectivity over normal cells. Longtime growth arrest was accompanied by senescence, where telomeric dysfunction is a predominant mechanism together with the accumulation of restricted DNA damage sites in the genome. Our data emphasize the potential of a senescence-mediated anticancer therapy through the use of G-quadruplex targeting small molecules based on the molecular framework of pyridostatin.
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