The bioreducible ruthenium(II) polypyridyl complexes (bRPCs) [(phen)2Ru(tatpp)]Cl2 (bRPC30) and [(phen)2Ru(tatpp)Ru(phen)2]Cl4 (bRPC40) (where tatpp is 9,11,20,22-tetraazatetrapyrido[3,2-a:2'3'-c:3'',2''-1:2''',3''']-pentacene) have been shown to cause DNA cleavage under aerobic and anaerobic conditions, have selective cytotoxicity and promising anti-tumor activity in mice. Their DNA cleavage activity is attributed to the redox activity of the tatpp ligand at modest (biologically accessible) reduction potentials. Structural variation of the redox-active ligand was performed, and the relationship of the redox activity of the modified complexes and their effectiveness to cleave DNA was investigated. This paper will present the development of novel related ruthenium(II) polypyridyl complexes consisting of varying aromatic bridging ligands and their structure-activity relationships as compared to the parent complexes bRPC30 and bRPC40.

Structure-activity relationships and DNA cleavage activity of bioreducible ruthenium(II) polypyridyl complexes

248th National Meeting (2014)

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