DNA-cleavage activity of the iron(II) complex with optically active ligands, meta- and para-xylyl-linked N′, N′-dipyridylmethyl-cyclohexane-1,2-diamine

DNA-cleavage agents such as bleomycin have potential anticancer applications. The development of a DNA-cleavage reagent that recognizes specific sequences allows the development of cancer therapy with reduced side effects. In this study, to develop novel compounds with specific DNA-cleavage activities, we synthesized optically active binuclear ligands, (1R,1'R,2R,2'R)-N-1,N-1'-(meta/para-phenylenebis(methylene))bis(N-2,N-2-bis (pyridin-2-ylmethyl)cyclohexane-1,2-diamine) and their enantiomers. The DNA-cleavage activities of these compounds were investigated in the presence of Fe(II)SO4 and sodium ascorbate. The obtained results indicated that the Fe(II) complexes of those compounds efficiently cleave DNA and that their cleavage was subtle sequence selective. Therefore, we succeeded in developing compounds that can be used as small-molecule drugs for cancer chemotherapy.

Automated summary

The study focuses on developing novel compounds with specific DNA-cleavage activities for cancer therapy. Experimental results indicate that the Fe(II) complexes of these compounds efficiently cleave DNA with subtle sequence selectivity. Therefore, these compounds have the potential to be used as small-molecule drugs for cancer chemotherapy.