Coordination-Driven Self-Assembly of Triazole-Based Apoptosis-Inducible Metallomacrocycles

Ru­(II)-metallomacrocycles containing
4-pyridyl-1,2,3-triazole moiety
were realized by coordination-driven self-assembly. All new compounds
were characterized by electrospray ionisation mass spectrometry, elemental
analysis, and 1H and 13C NMR spectroscopic techniques.
The molecular structure of metallomacrocycle 8 was determined
by single-crystal X-ray crystallography. The anticancer activities
of metallomacrocycles 5–8 were evaluated
by cytotoxicity, cell cycle analysis, and related protein expression.
Metallomacrocycle 7 showed the highest cytotoxicity in
HepG2 human hepatocellular carcinoma cells. In addition, apoptotic
HepG2 cells were analyzed when metallomacrocycle 7 was
treated. Our results suggest that metallomacrocycle 7 induces liver cancer cell death by increasing apoptosis and cell
cycle arrest and that it has potential use as an agent for the treatment
of human hepatocellular carcinoma.