%0 Journal Article
%T New Copper (II), Palladium (II), and Platinum (II) 2-Acetylpyrazine Tert-Butylthiosemicarbazone Complexes: Inhibition of Human Topoisomerase II¦Á and Activity against Breast Cancer Cells
%A Edward C. Lisic
%A Sarah N. Grossarth
%A Sarah B. Bowman
%A Jessica L. Hill
%A Michael W. Beck
%A Joseph E. Deweese
%A Xiaohua Jiang
%J Open Journal of Medicinal Chemistry
%P 1-13
%@ 2164-313X
%D 2022
%I Scientific Research Publishing
%R 10.4236/ojmc.2022.121001
%X 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<span> to be highly active against Gram positive
bacteria. The 4 compounds were also tested in human topoisomerase II<i>¦Á</i> DNA relaxation assays and all three
metal complexes had topoisomerase inhibition at a concentration between 4</span></span></span><span><span><span style=\"font-family:&quot;\"> </span></span></span><span><span><span style=\"font-family:&quot;\">-</span></span></span><span><span><span style=\"font-family:&quot;\"> </span></span></span><span><span><span style=\"font-family:&quot;\">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.</span></span></span><span><span><span style=\"font-family:&quot;\"> 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.
%K Topoisomerase
%K Breast Cancer
%K ¦Á-(N)-Heterocyclic Thiosemicarbazones
%U http://www.scirp.org/journal/PaperInformation.aspx?PaperID=117703