Thiosemicarbazone Ligands and their Metal Complexes; Compound Characterization and Topoisomerase II alpha Inhibitory Assays

Abstract

Thiosemicarbazone ligands and their metal complex have been seen to inhibit Topoisomerase II-α, a popular target of chemotherapy. This work demonstrates the synthesis and characterization of pyruvic aldehyde-1-oxime thiosemicarbazones: complex formation with Cu(II) and Pd(II). The compounds were then tested in a Topoisomerase II-α relaxation assay. The new thiosemicarbazone ligands, pyruvic aldehyde-1-oxime [x]-thiosemicarbazone (PAO-xTSC’s) and metal complexes have been synthesized. The ligands were characterized and analyzed by 1H Nuclear Magnetic Resonance spectrometry (NMR), 13C NMR, 1H13C HSQC, and 1H15N HSQC.