Carroll, W.R., Gardner, D.M., Melton, E.R., Murphy, S.T., Buckner, A.K., Fulmer, M.S., Qualls, W.G. and Lisic, E.C. (2018) 1H, 13C, and 15N NMR Conformational Characterization of a Series of 2-Acetylthiazolethiosemicarbazone Compounds. Journal of Molecular Structure, 1157, 8-13.
https://doi.org/10.1016/j.molstruc.2017.11.061

has been cited by the following article:

• TITLE: Cu(II) Propionyl-Thiazole Thiosemicarbazone Complexes: Crystal Structure, Inhibition of Human Topoisomerase IIα, and Activity against Breast Cancer Cells

  AUTHORS: Edward C. Lisic, Victoria G. Rand, Lana Ngo, Patrick Kent, Jeffrey Rice, Deidra Gerlach, Elizabeth T. Papish, Xiaohua Jiang

  KEYWORDS: Topoisomerase, Breast Cancer, Thiosemicarbazones

  JOURNAL NAME: Open Journal of Medicinal Chemistry, Vol.8 No.2, June 29, 2018

  ABSTRACT: 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 Cu2+ 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 IIα at activities between 2-4 μM for [Cu(PTZ-ETSC)Cl], and between 8-10 μM for the [Cu(PTZ-tBTSC)Cl] complex. The EC50 values for the MDA-MB-231 breast cancer cell line were 82.6 μM for (PTZ-ETSC), 17.9 μM for [Cu(PTZ- ETSC)Cl], 97.8 μM for (PTZ-tBTSC), and 1.41 μM for [Cu(PTZ-tBTSC)Cl]. The EC50 values for the MCF7 breast cancer cell lines were 9.36 μM for (PTZ-ETSC), 0.13 μM for [Cu(PTZ-ETSC)Cl], 0.333 μM for (PTZ-tBTSC), and 0.093 μM for [Cu(PTZ-tBTSC)Cl].