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Synthesis and application of mononuclear platinum (II) compounds as cytotoxic agents mimetics to cis - Platinum

机译:单核铂(II)化合物作为细胞毒性剂模拟物的合成及应用-顺铂

摘要

The present invention patent has the objective of a composition based on the synergetic effect of the organic compounds L1: 1 - {2 - (2 - (4-hydroxybenzyl piridilmetil) amino) - 3 - (1-naphthyloxy) - 2-propanol and L2: 1 - {2 -4-hydroxybenzyl (2 - piridilmetil) amino) - 3 - (2 - naftiloxi) - 2-propanol and salt of platinum K2 [PtCl4], for the subsequent production of cytotoxic agents similar to the drug cis platinum.Related to the area of medicinal inorganic chemistry. The present invention patent is applied to the pharmaceutical industry.Based on the results of the test cell viability (MTT)It is concluded that platinum compounds presented in this invention patent with high cytotoxic activity against all strains studied.Which is dependent on the structure of the organic binder.The compounds investigated were more cytotoxic to cancer cells than in normal human cells (PBMC), presenting selectivity similar to that of cisplatin.The results of labeling with annexin V and PI.Evaluation of cell cycle (sub G1) and measures the potential of mitochondrial membrane show that the type of death induced by complex 2 is necrosis and by complex 1 is apoptosis.With involvement of the mitochondria, indicating that the complex of platinum 1 is more promising in the development of new anticancer drugs.
机译:本发明专利的目的在于基于有机化合物L1的协同作用的组合物:1- {2-(2-(2-(4-羟基苄基哌啶子基)氨基)-3-(1-萘氧基)-2-丙醇和L2:1-{2 -4-羟基苄基(2-哌啶酮)氨基)-3-(2-萘甲酚)-2-丙醇和铂K2 [PtCl4]的盐,用于随后产生类似于顺式药物的细胞毒性剂铂。与药物无机化学领域有关。本发明专利应用于制药工业。基于测试细胞生存力(MTT)的结果,可以得出结论,本发明专利中提出的铂化合物对所有研究菌株均具有高细胞毒活性。被研究的化合物对癌细胞的细胞毒性比正常人细胞(PBMC)高,具有与顺铂相似的选择性.Annexin V和PI标记的结果。细胞周期的评估(sub G1)和措施线粒体膜的潜力表明复合物2诱导的死亡类型为坏死,复合物1诱导的死亡类型为细胞凋亡。随着线粒体的参与,表明铂1的复合物在新型抗癌药物的开发中更具前景。

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