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Copper (II) -Mixed Ligand Complexes with Anticancer Properties

机译:具有抗癌特性的铜(II)混合配体配合物

摘要

THE PRESENT INVENTION DISCLOSES PHARMACEUTICAL COMPOSITION HAVING AT LEAST ONE OF THE SERIES OF TERNARY COPPER(II) COMPLEXES, [CU(PHEN)(AA)(H2O)]NO3•xH2O 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 SELECTIVELY 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 GO/G1, PROTEASOME INHIBITION, OXIDATIVE DNA DAMAGE AND TOPOISOMERASE I (TOPO I) INHIBITION. MOST ILLUSTRATIVE DIAGRAM: FIGURE 1
机译:本发明公开了至少一种来自三价铜(II)络合物,来自1,10-邻苯二酚和氨基酸酸的[CU(PHEN)(AA)(AA)(H2O)] NO3•xH2O的药物组合物。所述氨基酸氨基酸配体为甘氨酸(GLY),SARCOSINE(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)配合物系列通过选择性地转移至癌细胞中来进一步表征。抗氧化剂的特性归因于活性氧物种(ROS)的产生,核双链DNA断裂(DSBs)的选择性诱导,GO / G1释放的细胞周期,蛋白质抑制,氧化性DNA损伤和拓扑异构酶I(I)。最具说明性的图:图1

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