The Square-Planar Cytotoxic [CuII(pyrimol)Cl] Complex Acts as an Efficient DNA Cleaver without Reductant

• DOI: 10.1021/ja056970+
• Publication Date: 2006-01-18T05:54:00Z
• Authors: Palanisamy Uma Ma...; Sudeshna Roy; Hans den Dulk; Sharief Barends; Gilles van Wezel; Bojan Kozlevčar; Patrick Gamez; Jan Reedijk
• Keywords: Ovarian Neoplasms; Mice; DNA, Superhelical; Cell Line, Tumor; Organometallic Compounds; Animals; Humans; Female; Cisplatin; Drug Screening Assays, Antitumor; Leukemia L1210; DNA Damage; 3. Good health

Chemical nucleases based on the transition-metal ions cleave DNA hydrolytically and/or oxidatively, with or without added reductant. We report here the novel DNA cleavage properties of the highly water-soluble, square-planar [Cu(Hpyrimol)Cl] complex, together with the results of cytotoxicities toward selected cancer cell lines. The copper complex cleaves PhiX174 supercoiled DNA efficiently without any reductant and shows high cytotoxicities toward L1210 murine leukemia and A2780 human ovarian carcinoma cancer cell lines that are sensitive and resistant to cisplatin. The IC50 values obtained for the copper complex in the sensitive cell lines are in the range of cisplatin, and for the cisplatin-resistant leukemia cell line, this value is even better.