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Morris, W.H., Ngo, L., Wilson, J.T., Medawala, W., Brown, A.R., Conner, J.D., Fabunmi, F., Cashman, D.J., Lisic, E.C., Yu, T., Deweese, J.E. and Jiang, X. (2019) Structural and Metal Ion Effects on Human Topoisomerase IIα Inhibition by α-(N)-Heterocyclic Thiosemicarbazones. Chemical Research in Toxicology, 32, 90-99.
https://doi.org/10.1021/acs.chemrestox.8b00204

has been cited by the following article:

• TITLE: New Copper (II), Palladium (II), and Platinum (II) 2-Acetylpyrazine Tert-Butylthiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against Breast Cancer Cells

  AUTHORS: Edward C. Lisic, Sarah N. Grossarth, Sarah B. Bowman, Jessica L. Hill, Michael W. Beck, Joseph E. Deweese, Xiaohua Jiang

  KEYWORDS: Topoisomerase, Breast Cancer, α-(N)-Heterocyclic Thiosemicarbazones

  JOURNAL NAME: Open Journal of Medicinal Chemistry, Vol.12 No.1, March 31, 2022

  ABSTRACT: The new ligand, 2-acetylpyrazine-tertbutylthiosemicarbazone (APZ-tBTSC), and its Cu(II), Pd(II) and Pt(II) complexes have been synthesized. This ligand coordinates to the metal ions in a tridentate monoanionic fashion forming monometallic complexes with the formula [M(APZ-tBTSC)Cl]. The ligand and the three metal complexes [Cu(APZ-tBTSC)Cl], [Pd(APZ-tBTSC)Cl], and [Pt(APZ-tBTSC)Cl] were tested for anti-proliferative biological behavior with a panel of seven microbes, and the copper and palladium complexes were found to be highly active against Gram positive bacteria. The 4 compounds were also tested in human topoisomerase IIα DNA relaxation assays and all three metal complexes had topoisomerase inhibition at a concentration between 4 - 6 micro-molar. The 4 compounds were also tested for activity with the HEK293T cell line and also the breast cell cancer line, MDA-MB-231. The most effective compound for activity against the HEK293T cell line was the [Cu(APZ-tBTSC)Cl] complex, and the MDA-MB-231 breast cancer cell line was the [Pt(APZ-tBTSC)Cl] complex.