Copper, tribromobis[μ-[methyl N-[di(2-pyridinyl-κN)methylene]carbonodithiohydrazonato-κN,κS']]tri-

Description

Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity.¹ It localizes to mitochondria and displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells (IC₅₀s = 0.74, 0.41, 0.62, and 2.06 μM, respectively). It induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells, effects that can be reduced by the ferroptosis inhibitor liproxstatin-1 . Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in the same cells. In vivo, complex 3 (1.5 and 3 mg/kg) reduces tumor volume and intratumor apoptosis in an AsPC-1 mouse xenograft model.

References

1. Guo, Y., Chen, M., Li, S., et al. Dithiocarbazate-copper complexes for bioimaging and treatment of pancreatic cancer J. Med. Chem. 64(9),5485-5499(2021).