The ruthenium(II) polypyridyl complex [(phen)2Ru(tatpp)Ru(phen)2]Cl4 (P ) has shown promising anti-tumor activity in mice. In vitro studies reveal that this complex binds and cleaves DNA in a manner that shows enhanced cleavage activity under low oxygen conditions (hypoxia).  It is known that the complex [Ru(phen)3]2+ and many simple derivatives are inhibitors of acetylcholinesterase (AChE), which can lead to neurotoxicity. In this paper, we study the inhibition of AChE by P  and some related complexes and relate this data to animal toxicity data. The ruthenium complexes examined include [(phen)2Ru(dppz)]Cl2, [(phen)2Ru(tpphz)]Cl2, [(phen)2Ru(tpphz)Ru(phen)2]Cl4, [(phen)2Ru(tatpp)]Cl2, [(Me4phen)2Ru(tatpp)]Cl2, [(Me4phen)2Ru(tatpp)Ru(Me4phen)2]Cl4, [(Ph2phen)2Ru(tatpp)]Cl2, [(Ph2phen)2Ru(tatpp)Ru(Ph2phen)2]Cl4, [Ru(Me4phen)3]Cl2, and [Ru(Ph2phen)3]Cl2. The enzyme inhibitory activity of the complexes were assessed and their IC50 values were obtained. This paper will discuss the structure-activity relationships with respect to AChE inhibition and toxicity.

Investigation of biological activity of ruthenium(II) polypyridyl complexes as inhibitors of acetylcholinesterase

245th National Meeting (2013)

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