A new pyrazolone based ternary Cu(II) complex: Synthesis, characterization, crystal structure, DNA binding, protein binding and anti-cancer activity towards A549 human lung carcinoma cells with a minimum cytotoxicity to non-cancerous cells

作者：Vyas Komal M; Jadeja R N^*; Patel Dipak; Devkar R V; Gupta Vivek K

来源：Polyhedron, 2013, 65: 262-274.

DOI：10.1016/j.poly.2013.08.051

• Pyrazolone based thiosemicarbazone
• Phenanthroline
• Ternary Cu(II) complex
• DNA binding
• Protein binding
• Anti-cancer activity

With the aim of exploring the anticancer properties of coordination compounds, we report for the first time the synthesis of the new ternary complex [Cu(TMCPMP-TS)(Phen)] (TMCPMP-TS; (Z)-2-((1-(3-chlorophenyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)(p-tolyl)methylene) hydrazinecarbothioamide and Phen; 1,10-phenanthroline). The complex was characterized by various techniques, including Xray crystallography which showed that the geometry of the metal centre was between square pyramidal and trigonal bipyramidal. The interaction with calf-thymus DNA showed binding through intercalation. The protein binding ability with bovine serum albumin revealed a stronger binding of complex as compared to the free ligands. The anticancer activity of the complex was investigated by exposing it to the A549 (human lung cancer) cell line, which showed mitochondrial damage via an oxidative mechanism. After 24 h treatment, the complex arrested S and G2/M phases in the cell cycle progression and induced cell death. The results envisaged herein indicate that Cu(TMCPMP-TS)(Phen) holds ample merit to develop it as a therapeutic agent against cancer.

• 出版日期2013-11-28