Gallium(III) complexes of α-N-heterocyclic piperidylthiosemicarbazones: Synthesis, structure-activity relationship, cellular uptake and activation of caspases-3/7/9

Add time:09/02/2019    Source:sciencedirect.com

Two types of α-N-heterocyclic piperidylthiosemicarbazone ligands and related Ga(III) complexes were synthesized. The structure of Ga4 and Ga5 were characterized by X-ray single crystal diffraction. We generated the related α-N-heterocycliperidinylthiosemicarbazone analogs to examine the effect of aldehydes or ketones in the Schiff base. The antitumor activity of both type ligands increased after coordination with gallium. Interestingly, the antitumor activity of gallium complexes containing pyridyl groups (first type ligands) is higher than that of pyrazine group-containing (second type ligands) complexes. Gallium complexes significantly depleted cellular iron, resulting in upregulation of transferrin receptor-1 and downregulation of ferritin. They also effectively activate the caspase family proteins (caspase-3/7/9), promote the release of cytochromes from the mitochondria, and ultimately lead to apoptosis.

We also recommend Trading Suppliers and Manufacturers of GALLIUM(III)-PHTHALOCYANINE CHLORIDE (cas 19717-79-4). Pls Click Website Link as below: cas 19717-79-4 suppliers

Prev:Research paperComplex formation reactions of gallium(III) and iron(III/II) with l-proline-thiosemicarbazone hybrids: A comparative study
Next:Arsenic (III, V), indium (III), and gallium (III) toxicity to zebrafish embryos using a high-throughput multi-endpoint in vivo developmental and behavioral assay)