Role of metalation in the topoisomerase IIα inhibition and antiproliferation activity of a series of α-heterocyclic-N4-substituted thiosemicarbazones and their Cu(II) complexes.

The topoisomerase-IIα inhibition and antiproliferative activity of α-heterocyclic thiosemicarbazones and their corresponding copper(II) complexes have been investigated. The CuII(thiosemicarbazonato)Cl complexes were shown to catalytically inhibit topoisomerase-IIα at concentrations (0.3–7.2 μM) over an order of magnitude lower than their corresponding thiosemicarbazone ligands alone. The copper complexes were also shown to inhibit the proliferation of breast cancer cells expressing high levels of topoisomerase-IIα (SK-BR-3) at lower concentrations than cells expressing lower levels of the enzyme (MCF-7).

已经对α-杂环缩氨基硫脲及其相应的铜（II）配合物的拓扑异构酶 - IIα抑制作用和抗增殖活性进行了研究。结果表明，CuII（缩氨基硫脲基）Cl配合物在浓度（0.3 - 7.2 μM）下对拓扑异构酶 - IIα的催化抑制作用比其相应的单独缩氨基硫脲配体低一个数量级以上。还表明铜配合物对高表达拓扑异构酶 - IIα的乳腺癌细胞（SK - BR - 3）的增殖抑制作用比对低表达该酶的细胞（MCF - 7）所需浓度更低。