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Updated: Oct 7, 2025

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Ru(III) complexes with pyrazolopyrimidines as anticancer agents: bioactivities and the underlying mechanisms
Yun-Qiong Gu1,2, Wen-Ying Shen1, Qi-Yuan Yang1
1State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Centre for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, P. R. China. chenzf@gxnu.edu.cn.
Abstract:
Three ruthenium(III) complexes with pyrazolopyrimidine [Ru(L)(H2O)Cl3] (1-3, n = 1-3) were prepared and characterized. These Ru(III) compounds show strong cytotoxicity against six cancer cell lines and low toxicity to normal human liver cells. Particularly, they exhibited stronger cytotoxicity to SK-OV-3 cells than cisplatin. Mechanism studies revealed that complex 1 inhibited tumor cell invasion and suppressed cell proliferation, induced apoptosis by elevating the levels of intracellular ROS (reactive oxygen species) and free calcium (Ca2+), and reduced mitochondrial membrane potential (ΔΨ). It also activated the caspase cascade, accompanied with upregulation of cytochrome c, Bax, p53, Apaf-1 and downregulation of Bcl-2. Moreover, complex 1 caused cell cycle arrest at S phase by inhibiting the expression of CDC 25, cyclin A2 and CDK 2 proteins, and induced DNA damage by interacting with DNA and inhibiting the topoisomerase I enzyme. Complex 1 exhibited efficient in vivo anticancer activity in a model of SK-OV-3 tumor xenograft.
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