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Abstract：
Three platinum(II) complexes of (1R,2R)-N(1)-cyclopentyl-1,2-cyclohexanediamine with malonate derivatives were designed, synthesized and spectrally characterized. MTT assay showed that the complexes possessed positive cytotoxic effect on the four human solid tumor cell lines. Among the complexes, complex 2 demonstrated the strongest cytotoxic activity compared to cisplatin and oxaliplatin against HepG2 cell line (IC50=3.04μM). Furthermore, the results of gel electrophoresis revealed that complex 2 interacted with DNA in a different mode from that of cisplatin. Mechanism studies of cell proliferation inhibition and cellular uptake indicated that complex 2 entered HepG2 cell more efficiently than cisplatin, exhibited massive G2 accumulation and then induced apoptosis.
摘要：
三铂（Ⅱ）配合物（1R，设计了2R-N(1)-环戊基-1,2-环己二胺与丙二酸酯衍生物,合成和光谱表征。MTT分析表明，该复合物对四种人实体瘤细胞系具有正的细胞毒性作用。在复合物中，与顺铂和奥沙利铂相比，复合物2对HepG2细胞系具有最强的细胞毒性活性（IC50=3.04μM）。此外，凝胶电泳结果表明，复合物2与DNA的相互作用方式与顺铂不同。细胞增殖抑制和细胞摄取的机制研究表明，复合物2比顺铂更有效地进入HepG2细胞。表现出大量的G2积累，然后诱导细胞凋亡。
