%0 Journal Article
%T Cu(II) Propionyl-Thiazole Thiosemicarbazone Complexes: Crystal Structure, Inhibition of Human Topoisomerase II¦Á, and Activity against Breast Cancer Cells
%A Edward C. Lisic
%A Victoria G. Rand
%A Lana Ngo
%A Patrick Kent
%A Jeffrey Rice
%A Deidra Gerlach
%A Elizabeth T. Papish
%A Xiaohua Jiang
%J Open Journal of Medicinal Chemistry
%P 30-46
%@ 2164-313X
%D 2018
%I Scientific Research Publishing
%R 10.4236/ojmc.2018.82004
%X Two new thiosemicarbazone ligands, 2-propionylthiazole ethylthiosemicarbazone (PTZ-ETSC), and 2-propionylthiazole tert-butylthiosemicarbazone (PTZ-tBTSC), along with their two copper(II) complexes, [Cu(PTZ-ETSC)Cl] and [Cu(PTZ-tBTSC)Cl], are reported here for the first time. Once characterized by NMR and MS, these mono-anionic tridentate ligands were reacted with Cu<sup>2+</sup> to form the square planar metal complexes [Cu(PTZ-ETSC)Cl] and [Cu(PTZ-tBTSC)Cl]. The x-ray crystal structure of the [Cu(PTZ-tBTSC)Cl] complex shows that the complex adopts a square planar arrangement around the copper(II) ion, but forms a sulfur-bridged dimer in the solid state. Both of the copper complexes displayed strong inhibition of human topoisomerase II¦Á at activities between 2-4 ¦ÌM for [Cu(PTZ-ETSC)Cl], and between 8-10 ¦ÌM for the [Cu(PTZ-tBTSC)Cl] complex. The EC50 values for the MDA-MB-231 breast cancer cell line were 82.6 ¦ÌM for (PTZ-ETSC), 17.9 ¦ÌM for [Cu(PTZ- ETSC)Cl], 97.8 ¦ÌM for (PTZ-tBTSC), and 1.41 ¦ÌM for [Cu(PTZ-tBTSC)Cl]. The EC50 values for the MCF7 breast cancer cell lines were 9.36 ¦ÌM for (PTZ-ETSC), 0.13 ¦ÌM for [Cu(PTZ-ETSC)Cl], 0.333 ¦ÌM for (PTZ-tBTSC), and 0.093 ¦ÌM for [Cu(PTZ-tBTSC)Cl].
%K Topoisomerase
%K Breast Cancer
%K Thiosemicarbazones
%U http://www.scirp.org/journal/PaperInformation.aspx?PaperID=85714