New Copper (II), Palladium (II), and Platinum (II) 2-Acetylpyrazine Tert-Butylthiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against Breast Cancer Cells

Edward C. Lisic; Sarah N. Grossarth; Sarah B. Bowman; Jessica L. Hill; Michael W. Beck; Joseph E. Deweese; Xiaohua Jiang

首页> 中文期刊> 《药物化学期刊（英文）》 >New Copper (II), Palladium (II), and Platinum (II) 2-Acetylpyrazine Tert-Butylthiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against Breast Cancer Cells

New Copper (II), Palladium (II), and Platinum (II) 2-Acetylpyrazine Tert-Butylthiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against Breast Cancer Cells

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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 to be highly active against Gram positive bacteria. The 4 compounds were also tested in human topoisomerase IIα DNA relaxation assays and all three metal complexes had topoisomerase inhibition at a concentration between 4 - 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. 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.

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《药物化学期刊（英文）》 |2022年第1期|1-13|共13页
作者
Edward C. Lisic; Sarah N. Grossarth; Sarah B. Bowman; Jessica L. Hill; Michael W. Beck; Joseph E. Deweese; Xiaohua Jiang;
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作者单位

Department of Chemistry;

Tennessee Technological University;

Cookeville;

TN;

USA;

Department of Biological;

Physical and Human Sciences;

Freed Hardeman University;

Henderson;

TN;

USA;

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原文格式 PDF
正文语种 chi
中图分类有机化学;
关键词
TOPOISOMERASE; Breast Cancer; α-(N)-Heterocyclic Thiosemicarbazones;

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New Copper (II), Palladium (II), and Platinum (II) 2-Acetylpyrazine Tert-Butylthiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against Breast Cancer Cells

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