AI Article Synopsis
- Recent research has focused on biscationic compounds for their potential antitumor properties, specifically targeting ChoK inhibitors and evaluating effectiveness against various cancer cell lines.* -
- A new family of bromide compounds (9a-k), which include nitrogen atoms that could potentially serve as hydrogen bond acceptors, was synthesized and tested for anticancer activity.* -
- Among these, compounds 9g-i showed the most significant ability to inhibit cancer cell growth, particularly in leukemia, even at very low concentrations, and compound 9h was noted for its ability to induce cell death through the mitochondrial pathway.*
Article Abstract
Aim: Research of the antitumor properties of biscationic compounds has received significant attention over the last few years.
Results: A novel family of 1,1'-([2,2'-bipyridine]-5,5'-diylbis(methylene))bis-substituted bromide (9a-k), containing two nitrogen atoms in the linker, considered as hypothetical hydrogen bond acceptors, were synthesized and evaluated as ChoK inhibitors and their antiproliferative activity against six cancer cell lines.
Conclusion: The most promising compounds in this series are 1,1'-([2,2'-bipyridine]-5,5'-diylbis(methylene))bis(4-(methyl(phenyl)amino)-quinolinium bromide derivatives 9g-i (analogs to RSM932A), that significantly inhibit cancer cell growth at even submicromolar concentrations, especially against leukemia cells. Compounds 9g-i also inhibit the ChoKα1 with good or moderate values, as predicted by initial docking studies. In addition, the most active compound 9h remarkably induces apoptosis in two cell lines following the mitochondrial pathway.
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| http://dx.doi.org/10.4155/fmc.15.1 | DOI Listing |
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