Date of Award
Master of Science (MS)
Department of Chemistry
Michael I. Webb
Platinum-based drugs have over the years been administered in the treatment of tumours.
Unfortunately, platinum resistance and the severe side effects associated with the treatments has necessitated the research for new anti-cancer drugs. Ruthenium(II) and Ruthenium(III) complexes have shown promise as useful alternative anticancer agents. The lead candidates include the Ru(II) complex RAPTA-C, a ruthenium(II)-arene complex [Ru(η6-p-cymene)Cl2(1,3,5-triaza-7-phosphaadamantane)] and the Ru(III) complex NAMI-A [imidazoleH][trans-Ru(imidazole) (dimethyl sulfoxide)Cl4]. Both compounds have shown potent cytotoxic activity in several primary human tumor models. Unfortunately, NAMI-A could not advance in clinical evaluations due to limited efficacy in vivo, while the clinical evaluation of RAPTA-C is unknown. Therefore, there is a need for novel cancer therapeutics that have high biological activity, are relatively easy to synthesize, and can readily be modified. This work focuses on the use of 2-acetylpyridine and 2-pyridinecarboxaldehyde for the synthesis, characterization, and preliminary evaluation of derivatives of both the RAPTA-C and NAMI-A anticancer complexes containing Schiff base ligands. Here, the results of the synthesis of these compounds and their subsequent characterization using 1H NMR, MS, fluorescence and UV-Vis spectroscopies are presented.
Mensah, Stephen, "Syntheses, Characterization, and Preliminary Evaluation of Potential Ruthenium Anticancer Complexes Containing Schiff Base Ligands" (2019). Theses and Dissertations. 1164.