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首页> 外文期刊>Anticancer Research: International Journal of Cancer Research and Treatment >Synthesis and antitumour activity of a new trinuclear platinum compound [{cis-PtCl(NH3)2μ {trans-Pt(3-hydroxypyridine)2H2N(CH2)5NH2)2}] Cl4 in human ovarian cancer cells.
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Synthesis and antitumour activity of a new trinuclear platinum compound [{cis-PtCl(NH3)2μ {trans-Pt(3-hydroxypyridine)2H2N(CH2)5NH2)2}] Cl4 in human ovarian cancer cells.

机译：新的三核铂化合物的合成和抗肿瘤活性[{CIS-PTCL（NH 3）2μ{Trans-Pt（3-羟基吡啶）2H2N（CH2）5NH2）2}] Cl4在人卵巢癌细胞中。

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摘要

A trinuclear platinum compound with a cis-geometry for the terminal metal centers coded as QH5 has been synthesized and investigated for activity against the human ovarian A2780, A2780(cisR) and A2780(ZD0473R) cancer cell lines. Cellular accumulation of platinum, level of platinum-DNA binding and nature of interaction of the compound with pBR322 plasmid DNA have also been determined. QH5 is found to be more active than cisplatin against all the three cell lines and to have much lower resistant factors than cisplatin. The compound is 2.5-times more active than cisplatin against the A2780(cisR) cell line and 11.5-times more active than cisplatin against A2780(ZD0473R) cell line. When the activity of QH5 in A2780 cell line is compared with its activity in the A2780(ZD0473R) cell line, it is found to be 2.4-times more active against the resistant A2780(ZD0473R) cancer cell line than the parent A2780 cell line, thus indicating that it has been able to overcome mechanisms of resistance operating in the A2780(ZD0473R) cell lines. The higher activity of QH5 as compared to cisplatin is found to be associated with higher platinum accumulation at all time points and high level of platinum-DNA binding at 24 h in all the three human ovarian cancer cell lines. Provided QH5 has the right toxicity profile and its in vitro activity is complemented with sufficient activity in vivo, the compound may have the potential for development as a novel platinum-based anticancer drug targeted to ovarian cancer.
机译：已经合成了与作为QH5编码的末端金属中心的CIS-几何形状的三核铂化合物，并研究了针对人卵巢A2780，A2780（CISR）和A2780（ZD0473R）癌细胞系的活性。还确定了铂的细胞积聚，铂 - DNA与PBR322质粒DNA的铂-DNA结合和性质的性质也得到了测定。发现QH5比SISplatin对所有三种细胞系更活跃，并且具有比顺铂更低的抗性因素。该化合物比顺铂更活跃2.5倍，与A2780（CISR）细胞系相对于A2780（CISR）细胞系，比顺铂更高的11.5倍，与A2780（ZD0473R）细胞系相对顺铂。当A2780细胞系中QH5的活性与其在A2780（ZD047R）细胞系中的活性进行比较时，发现与耐母A2780细胞系相比抗性A2780（ZD0473R）癌细胞系数比较有效的2.4倍。因此，表明它能够克服在A2780（ZD0473R）细胞系中运行的电阻的机制。发现与顺铂相比QH5的较高活性与在所有三种人卵巢癌细胞系中，在24小时的所有时间点和高水平的铂-DNA结合时与铂积累的较高铂积累相关。提供QH5具有良好的毒性型材，其体外活性与体内足够的活性互补，该化合物可能具有旨在作为卵巢癌的新型铂族抗癌药物的发展潜力。

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