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首页> 外文期刊>Archiv der Pharmazie >Platinum Complexes with 5-Methyl-5(4-pyridyl)hydantoin and Its 3-Methyl Derivatives: Synthesis and Cytotoxic Activity – Quantitative Structure-Activity Relationships
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Platinum Complexes with 5-Methyl-5(4-pyridyl)hydantoin and Its 3-Methyl Derivatives: Synthesis and Cytotoxic Activity – Quantitative Structure-Activity Relationships

机译:5-甲基-5(4-吡啶基)乙内酰脲及其3-甲基衍生物的铂配合物:合成和细胞毒性活性-定量结构-活性关系

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摘要

3,5-Dimethyl-5-(4-pyridyl)hydantoin (L) and its platinum(II) and platinum(IV) complexes with the general formula cis-[PtL2X2]?·?n H2O and [PtL2Cl4], where XCl, I and n?=?2-4 were synthesized. A new Pt(IV) complex with 5-methyl-5-(4-pyridyl)hydantoin (L′) with the formula cis-[Pt(L′)2Cl2(OH)2]?·?5 H2O was also synthesized. The novel compounds were characterized by elemental analysis, IR, 1H-, 13C-, 195Pt-NMR spectra and molar conductivity. The cytotoxic effects of these complexes were examined on three human tumor cell lines by MTT-dye reduction assay. These four new Pt(II) and Pt(IV) complexes and a set of another twelve Pt(II), Pt(IV), and Pd(II) complexes previously synthesized and tested were compiled and a QSAR model was derived in order to direct the further rational synthesis.
机译:3,5-二甲基-5-(4-吡啶基)乙内酰脲(L)及其通式为cis- [PtL 2 X 2的铂(II)和铂(IV)配合物]?·?n H 2 O和[PtL 2 Cl 4 ],其中XCl,I和n?=?合成2-4。一种新的具有5-甲基-5-(4-吡啶基)乙内酰脲(L')的Pt(IV)配合物,其化学式为cis- [Pt(L') 2 Cl 2 (OH) 2 ]?·?5 H 2 O。通过元素分析,IR, 1 H-, 13 C-, 195 Pt-NMR谱和摩尔电导率对其进行表征。通过MTT染料还原测定法检查了这些复合物对三种人肿瘤细胞系的细胞毒性作用。编译这四个新的Pt(II)和Pt(IV)配合物以及之前合成和测试的另外十二种Pt(II),Pt(IV)和Pd(II)配合物,并导出QSAR模型以指导进一步的理性综合。

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