Presentation Title

Synthesis and Characterization of Ruthenium Complexes Containing Modified Terpyridine and Chloroquine Analogue Ligands: Reactivity with DNA

Start Date

November 2016

End Date

November 2016

Location

HUB 268

Type of Presentation

Oral Talk

Abstract

The discovery of cis-platin as a chemotherapeutic agent has pioneered the search for a less toxic and more efficient anti-cancer drug within the domain of inorganic chemistry. Ruthenium complexes have had quite the spotlight in this search due to their beneficial chemical and biological properties, such as a variety of stable oxidation states, preference for six-coordinate geometry, and compatibility with biological fluids. In fact, NAMI-A and KP1019--both of which are ruthenium complexes--have made it to the clinical trial stage in anti-cancer drug development. Ligands of the polypyridyl class have shown promise in the production of anti-cancer drugs due to their intercalative capabilities. Chloroquine has had some attention in the anti-cancer spotlight, specifically with inducing apoptosis in several tumor cell lines of glioma and arene-ruthenium complexes of chloroquine which have exhibited the induction of apoptosis upon multiple cell lines. In this project, the DNA reactivities have been studied for a new ruthenium complex of the general formula: Ru(x-tpy)(Y)(L), where x is the modification of the terpyridine ligand (x=hydrogen, phenyl, tolyl, methoxyphenyl), Y is either a -chloro or -aquo ligand, and L is the chloroquine analogue ligand. All synthesized complexes and ligands have been characterized by spectroscopic techniques. Through absorption titration and competitive binding studies with ethidium bromide, the Ksv binding constants of some of the complexes have been determined. Overall, the binding constants are within the magnitude of 105 and 104 for absorption titration and competitive binding, respectively, suggesting that the complexes bind fairly strongly to DNA.

Keywords: Anticancer drugs, ruthenium complexes, DNA binding, CT DNA, terpyridine

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Nov 12th, 2:45 PM Nov 12th, 3:00 PM

Synthesis and Characterization of Ruthenium Complexes Containing Modified Terpyridine and Chloroquine Analogue Ligands: Reactivity with DNA

HUB 268

The discovery of cis-platin as a chemotherapeutic agent has pioneered the search for a less toxic and more efficient anti-cancer drug within the domain of inorganic chemistry. Ruthenium complexes have had quite the spotlight in this search due to their beneficial chemical and biological properties, such as a variety of stable oxidation states, preference for six-coordinate geometry, and compatibility with biological fluids. In fact, NAMI-A and KP1019--both of which are ruthenium complexes--have made it to the clinical trial stage in anti-cancer drug development. Ligands of the polypyridyl class have shown promise in the production of anti-cancer drugs due to their intercalative capabilities. Chloroquine has had some attention in the anti-cancer spotlight, specifically with inducing apoptosis in several tumor cell lines of glioma and arene-ruthenium complexes of chloroquine which have exhibited the induction of apoptosis upon multiple cell lines. In this project, the DNA reactivities have been studied for a new ruthenium complex of the general formula: Ru(x-tpy)(Y)(L), where x is the modification of the terpyridine ligand (x=hydrogen, phenyl, tolyl, methoxyphenyl), Y is either a -chloro or -aquo ligand, and L is the chloroquine analogue ligand. All synthesized complexes and ligands have been characterized by spectroscopic techniques. Through absorption titration and competitive binding studies with ethidium bromide, the Ksv binding constants of some of the complexes have been determined. Overall, the binding constants are within the magnitude of 105 and 104 for absorption titration and competitive binding, respectively, suggesting that the complexes bind fairly strongly to DNA.

Keywords: Anticancer drugs, ruthenium complexes, DNA binding, CT DNA, terpyridine