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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Efficient one-pot synthesis of trans-Pt(II)-(salicylaldimine)(4-picoline)Cl complexes: effective agents for enhanced expression of p53 tumor suppressor genes
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Efficient one-pot synthesis of trans-Pt(II)-(salicylaldimine)(4-picoline)Cl complexes: effective agents for enhanced expression of p53 tumor suppressor genes

机译:有效的一锅合成反式Pt(II)-(水杨醛亚胺)(4-甲基吡啶)Cl复合物:增强p53抑癌基因表达的有效药物

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摘要

A series of trans-Pt(II)(salicylaldimine)(4-picoline)Cl complexes were synthesized in 78-87% yield using a one-pot procedure from commercially available precursors. The structures of these complexes were characterized by H-1, F-19 and C-13 NMR spectroscopy, HRMS (ESI) as well as single crystal X-ray analysis. Bioactivity investigations including bio-assay, time-and dose-dependent, cell cycle progression study, caspase 3 and 9 apoptosis marker assay and DNA interaction using pBR322 plasmid DNA by gel electrophoresis were performed. The results indicated that the complexes showed promising in vitro cytotoxicity in MCF-7 and A549 cancer cell lines. Moreover these complexes enhanced the expression of p53 tumor suppressor gene family members such as p63 and p73.
机译:使用一锅法从市售前体中合成了一系列反式Pt(II)(水杨醛亚胺)(4-甲基吡啶)Cl络合物,收率为78-87%。这些配合物的结构通过H-1,F-19和C-13 NMR光谱,HRMS(ESI)以及单晶X射线分析来表征。进行了生物活性研究,包括生物测定,时间和剂量依赖性,细胞周期进程研究,胱天蛋白酶3和9凋亡标记物测定以及使用pBR322质粒DNA通过凝胶电泳进行DNA相互作用。结果表明,该复合物在MCF-7和A549癌细胞系中显示出有希望的体外细胞毒性。而且,这些复合物增强了p53肿瘤抑制基因家族成员如p63和p73的表达。

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