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首页> 外文期刊>Chemical and Pharmaceutical Bulletin >Synthesis, characterization and biological evaluation of platinum(II) complexes with a chiral N-monosubstituted 1,2-cyclohexyldiamine derivative
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Synthesis, characterization and biological evaluation of platinum(II) complexes with a chiral N-monosubstituted 1,2-cyclohexyldiamine derivative

机译:带有手性N-单取代的1,2-环己基二胺衍生物的铂(II)配合物的合成,表征和生物学评价

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摘要

Eight platinum(II) compounds with a new chiral ligand, 2-(((1R,2R)-2- aminocyclohexylamino)methyl)phenol (HL), were designed, prepared and spectrally characterized. All compounds showed better aqueous solubility than cisplatin and oxaliplatin. In vitro cytotoxicity of these compounds against human HepG-2, MCF-7, A549 and HCT-116 cell lines was evaluated. Results indicated that all compounds showed cytotoxicity against A549 and HepG-2 cell lines. Particularly, compounds B1 and B8, which have CF3SO3- and (CH3)3COCH2COO- as leaving groups, respectively, exhibited better cytotoxicitiy than that of carboplatin in these two cell lines.
机译:设计,制备并光谱表征了具有新手性配体2-((((1R,2R)-2-氨基环己基氨基)甲基)苯酚(HL)的八种铂(II)化合物。所有化合物均显示出比顺铂和奥沙利铂更好的水溶性。评估了这些化合物对人HepG-2,MCF-7,A549和HCT-116细胞系的体外细胞毒性。结果表明,所有化合物均显示出对A549和HepG-2细胞系的细胞毒性。特别地,分别具有CF 3 SO 3和(CH 3)3 COCH 2 COO-作为离去基团的化合物B 1和B 8在这两个细胞系中显示出比卡铂更好的细胞毒性。

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