首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Novel trans-dichloridoplatinum(II) complexes with 3- and 4-acetylpyridine: Synthesis, characterization, DFT calculations and cytotoxicity.
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Novel trans-dichloridoplatinum(II) complexes with 3- and 4-acetylpyridine: Synthesis, characterization, DFT calculations and cytotoxicity.

机译:具有3-和4-乙酰吡啶的新型反式二氯铂(II)配合物:合成,表征,DFT计算和细胞毒性。

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摘要

Novel complexes of platinum(II) with 3- (1) or 4-acetylpyridine (2) have been synthesized and characterized by elemental analyses, IR, (1)H and (13)C NMR spectroscopy. Single crystal X-ray diffraction revealed the trans geometry of complex 2. DFT calculations confirm formation of trans isomers for both complexes. The complexes have been tested for their cytotoxicity against HeLa (human cervical cancer), U2OS (human osteosarcoma), U2OScisR (human osteosarcoma cisplatin resistant), B16 (murine melanoma), MDA-453, MDA-361, and MCF-7 (human breast cancer), LS-174 (human colon cancer) and FemX (human melanoma) cell lines. The most promising compound trans-dichloridobis(4-acetylpyridine)platinum(II) (2) overcomes cisplatin resistance of U2OScisR cells after 48h of drug exposure.
机译:铂(II)与3-(1)或4-乙酰基吡啶(2)的新型配合物已合成,并通过元素分析,IR,(1)H和(13)C NMR光谱进行了表征。单晶X射线衍射揭示了配合物2的反式几何形状。DFT计算证实了两种配合物的反式异构体的形成。已测试了该复合物对HeLa(人类宫颈癌),U2OS(人类骨肉瘤),U2OScisR(人类骨肉瘤顺铂耐药),B16(鼠黑色素瘤),MDA-453,MDA-361和MCF-7(人类)的细胞毒性乳腺癌,LS-174(人类结肠癌)和FemX(人类黑色素瘤)细胞系。最有前途的化合物反式二氯双(4-乙酰基吡啶)铂(II)(2)在药物暴露48小时后克服了U2OScisR细胞的顺铂耐药性。

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