Previous studies demonstrated that HDpT chelators have potent
anti-tumour activity. We have now designed and generated two new
groups of chelators, HBpT and HNBpT. Comparing the three series of
chelators, the HBpT analogues displayed highest anti- proliferative
efficacy against SK-N-MC neuroepithelioma cells and was greater
than other well known chelators (DFO, Triapine and 311). Three
analogues of the HBpT series displayed much greater
anti-proliferative activity against SK-N-MC cells than normal MRC-5
fibroblasts, indicating their selectivity against tumour cells.
Structure-activity relationships examination demonstrated that
lipophilicity and redox cycling activity were important factors in
generating potent chelators. Redox activity determined by ascorbate
oxidation and benzoate hydroxylation assays showed that the HBpT
ligands were the most active chelators. Microarray studies using
DFO and HDp44mT, demonstrated up- regulation of the gene in cell
cycle arrest, while genes in cancer progression were
down-regulated. The current studies have identified a novel group
of chelators with the greatest activity of all chelators previously
prepared in our lab.
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