Biological Activity of a Series of Bis(thiosemicarbazone) Bis(alkylthiocarbamate) and Thiosemicarbazone-alkylthiocarbamate Hybrid Cu Complexes

Since 2015, I have been engaged in a collaboration between Professor Craig Grapperhaus and Professor Paula Bates (Department of Medicine at UofL) to prepare and evaluate the antiproliferation activity of a series of Cu complexes of bis(dithiosemicarbazone), bis(alkylthiocarbamate), and thiosemicarbazone-alkyldithiocarbamate ligands. We have identified a small library of complexes with high antiproliferation activity and high solid tumor selectivity. We are current conducting structure-activity studies and identification of mechanism of action. Representative and informative articles on our studies are listed below.

A new hybrid thiosemicarbazone−alkylthiocarbamate ligand system has been successfully synthesized, and corresponding Cu, Ni, and Zn complexes have been prepared and their antiproliferation activity against lung adenocarcinoma cells evaluated by MTT a

Citations

S. A. Andres, K. Bajaj, N. S. Vishnosky, M. A. Peterson, M. S. Mashuta, R. M. Buchanan, P. J. Bates, C. A. Grapperhaus, “Synthesis, Characterization, and Biological Activity of Hybrid Thiosemicarbazone-Alkylthiocarbamate Metal Complexes" Inorg. Chem. 2020, 59, 4924-4935. doi:10.1021/acs.inorgchem.0c00182.

 

Grapperhaus CA, Buchanan RM, Vishnosky NS, Young JO, Bates PJ, Andres SA, Calvary CA, inventors; University of Louisville Research Foundation ULRF, assignee. Compounds, compositions, methods for treating diseases, and methods for preparing compounds. United States patent US 11,208,379. 2021 Dec 28.

 

K. Bajaj, S. A. Andres, D. T. Hofsommer, M. Galib, M. S. Mashuta, B. Bennett, B. Narayanan, R. M. Buchanan, P. J. Bates, C. A. Grapperhaus, “Investigations of Bis (alkylthiocarbamato) copper Linkage Isomers.” Inorganic Chemistry. 2022 May 12.

 

K. Bajaj, R. M. Buchanan, C. A. Grapperhaus, “Antifungal activity of thiosemicarbazones, bis (thiosemicarbazones), and their metal complexes.” Journal of Inorganic Biochemistry. 2021 Dec 1;225:111620.