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Synthesis, cytotoxicity, and apoptosis induction study of antitumor dinuclear platinum(II) complexes

机译:抗肿瘤双核铂(II)配合物的合成,细胞毒性和凋亡诱导研究

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摘要

Five novel dinuclear platinum(II) complexes with a new chiral ligand, 3-(2-amino-cyclohexylamino)-propionic acid (HP), were designed, prepared and spectrally characterized. The in vitro cytotoxicities of these compounds were evaluated against the HepG-2, MCF-7, A549, and HCT-116 cell lines. The results indicated that all compounds showed cytotoxicity towards the HepG-2 cell line. Particularly, complex X5, which has SO 42- as a bridge, exhibited better cytotoxicity than carboplatin or oxaliplatin against all selected cell lines. Moreover, double dyeing flow cytometric resection indicated that the target compounds inhibited tumor cell growth by inducing apoptosis. Five novel dinuclear platinum(II) complexes with a new chiral ligand, 3-(2-amino- cyclohexylamino)-propionic acid, were designed. The in vitro cytotoxicity results of these compounds against the HepG-2, MCF-7, A549, and HCT-116 cell lines indicated that all compounds showed cytotoxicity towards the HepG-2 cell line. Particularly, complex X5, which has SO 42- as a bridge, exhibited better cytotoxicity than carboplatin or oxaliplatin against all selected cell lines.
机译:设计,制备和光谱表征了五个具有新的手性配体3-(2-氨基-环己基氨基)-丙酸(HP)的新型双核铂(II)配合物。评估了这些化合物对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HepG-2细胞系的细胞毒性。特别地,具有SO 42-作为桥的络合物X5对所有选择的细胞系表现出比卡铂或奥沙利铂更好的细胞毒性。此外,双染色流式细胞术切除表明目标化合物通过诱导凋亡来抑制肿瘤细胞的生长。设计了五种具有新手性配体3-(2-氨基-环己基氨基)-丙酸的新型双核铂(II)配合物。这些化合物对HepG-2,MCF-7,A549和HCT-116细胞系的体外细胞毒性结果表明,所有化合物均对HepG-2细胞系显示出细胞毒性。特别地,具有SO 42-作为桥的络合物X5对所有选择的细胞系表现出比卡铂或奥沙利铂更好的细胞毒性。

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