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COPPER(II) -MIXED LIGAND COMPLEXES WITH ANTICANCER PROPERTIES

机译:具有抗氧化剂特性的铜(II)混合配体

摘要

The present invention discloses pharmaceutical composition having at least one of the series of ternary copper(II) complexes, [Cu(phen)(aa)(H2O)]ΝO3·xΗ2O from 1,10-phenanthroline and amino acid ligands. The said amino acid ligands are glycine (gly), sarcosine (sar), DL-alanine (DL-ala), or 2, 2-dimethylglycine (C-dMg). The series of ternary copper(II) complexes with anticancer properties are further characterized by selectivity towards cancer cells. The anticancer properties are due to increase reactive oxygen species (ROS) generation, selective induction of nuclear double strand DNA breaks (DSBs), cell cycle arrested at G0/G1, proteasome inhibition, oxidative DNA damage and topoisomerase I (topo I) inhibition.
机译:本发明公开了具有至少一系列三元铜(II)配合物,[Cu(phen)(aa)(H 2 O)] NO 3 ·xH 2 O。所述氨基酸配体是甘氨酸(gly),肌氨酸(sar),DL-丙氨酸(DL-ala)或2,2-二甲基甘氨酸(C-dMg)。具有抗癌特性的三元铜(II)配合物系列进一步以对癌细胞的选择性为特征。抗癌特性归因于活性氧(ROS)的产生增加,核双链DNA断裂(DSBs)的选择性诱导,细胞周期停滞在G 0 / G 1 ,蛋白酶体抑制,氧化性DNA损伤和拓扑异构酶I(拓扑I)抑制。

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