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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Three cobalt(II) complexes containing pyrimidylanthrahydrazone ligands: Synthesis, crystal structure, DNA binding,
Jia-Yu Xu1, Xue-Bin Bi1, Sha-Sha Luo1
1Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Guangxi Key Laboratory of Chemistry and Molecular Engineering of Medicinal Resources, University Engineering Research Center for Chemistry of Characteristic Medicinal Resources (Guangxi), School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, China.
Abstract:
This research presents the design, synthesis, structural characterization, and evaluation of the anticancer activities of three new pyrimidylanthrahydrazone cobalt(II) complexes: 1) 9-MPMAH-Co, 2) 9-FPMAH-Co, and 3) 9-PMAH-Co. Single-crystal X-ray diffraction analysis confirmed that all three complexes adopt a hexacoordinate mononuclear geometry. However, differences in their coordination modes were observed due to variations in the ligand substituents (-CH3, -F, -H). Spectroscopic DNA interaction studies indicated that all three cobalt complexes exhibit varying levels of DNA intercalation. Topoisomerase I inhibition assays revealed that 9-PMAH-Co demonstrates significant enzyme inhibition at a low concentration of 1 μM. In vitro antiproliferative assays confirmed that 9-PMAH-Co exhibits potent cytotoxic activity against SK-OV-3 and HeLa-229 cancer cell lines, with IC₅₀ values of 4.99 ± 0.18 μM and 8.09 ± 1.13 μM, respectively, while showing reduced toxicity toward normal liver cells (HL-7702) compared to cisplatin. Further investigation through cell cycle analysis indicated that 9-PMAH-Co induces G2/M phase arrest in SK-OV-3 cells, with a population increase to 91.37 % (Δ = 76.59 %). Studies on the structural-activity relationship suggest that the synergistic interactions between the ligand substituents and the cobalt center play a crucial role in modulating biological activity, highlighting 9-PMAH-Co as a promising lead compound for the development of targeted anticancer agents.
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