Synthesis, antiproliferative activity and mechanism of gallium(III)-thiosemicarbazone complexes as potential anti-breast cancer agents

European Journal of Medicinal Chemistry
Jinxu QiYihong Wang

Abstract

Five thiosemicarbazone ligands were synthesized and characterized by condensation with different aldehydes or ketones by 4-phenylthiosemicarbazone. The representative dichlorido[2-(Di-2-pyridinylmethylene)-Nphenylhydrazinecarbothioamide-N,N,S]-gallium(III) (Ga4) was characterized by X-ray single crystal diffraction, which was 1:1 ligand/Ga(III) complexes. The structure-activity relationship of these ligands and Ga (III) complexes have been investigated, and the results demonstrate that the formation of Ga (III) complexes have significant antiproliferative activity over the corresponding ligands. The anticancer mechanism of gallium (III) complexes has been studied in detail, which is typical agents that effect on the mitochondrial apoptotic pathway. The ability of gallium (III) complexes to inhibit the cell cycle does not enhanced with the increasing concentrations, whereas the ability to promote apoptosis is concentration-dependent.

Citations

Apr 4, 2020·Dalton Transactions : an International Journal of Inorganic Chemistry·Débora E S SilvaAdelino V G Netto
Oct 1, 2019·Dalton Transactions : an International Journal of Inorganic Chemistry·Fanghui ChenBaiwang Sun
Nov 25, 2020·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Weidong FeiCaihong Zheng
Apr 4, 2021·Pharmaceutics·Minja MladenovićNikola Ž Knežević

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