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

Jatinder Singh; Dae Won Park; Dong Hwan Kim; Nem Singh; Se Chan Kang; Ki-Whan Chi

doi:10.1021/acsomega.9b00093

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

ACS Omega. 2019 Jun 21;4(6):10810-10817. doi: 10.1021/acsomega.9b00093. eCollection 2019 Jun 30.

Authors

Jatinder Singh¹, Dae Won Park², Dong Hwan Kim¹, Nem Singh¹, Se Chan Kang², Ki-Whan Chi¹

Affiliations

¹ Department of Chemistry, University of Ulsan, Ulsan 44776, Republic of Korea.
² Department of Oriental Medicine Biotechnology, College of Life Sciences, Kyung Hee University, Yongin 17104, Republic of Korea.

Abstract

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.