Synthesis, GC selective DNA binding and topoisomerase II inhibition activities of ruthenium(II) polypyridyl complex containing 11-aminopteridino [6,7-f][1,10]phenanthrolin-13(12H)-one

A DNA-intercalating Ru(II) polypyridyl complex [Ru(bpy)(2)(appo)](2+) (bpy=2,2'-bipyridine, appo = 11-aminopteridino[6,7-f][1,10]phenanthrolin-13(12H)-one) has been synthesized and characterized by elemental analysis, electrospray mass spectra, H-1 NMR, UV/Vis spectrum, fluorescent spectrum and electrochemistry. The DNA-binding, photocleavage, and topoisomerase inhibition of the complex was studied. Interestingly, the complex binds to DNA via an intercalative mode with preference for GC sequences and cleaves the pBR322 DNA upon irradiation. In addition, the complex shows high inhibition activity against topoisomerase II by interfere the DNA religation. (C) 2008 Elsevier Inc. All rights reserved.