新型顺铂和卡铂类似物的合成及其体外细胞毒活性的初步研究。

Drug design and discovery Pub Date : 1998-10-01
A Séné, G Bérubé, R C Gaudreault
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引用次数: 0

摘要

以三苯基乙烯为原料,以不同的二胺为原料合成了六个新的铂(II)配合物。在人乳腺癌细胞系(MCF-7和MDA-MB-231)上评估的化合物的细胞毒性受到二胺配体性质的很大影响。两种衍生物的细胞毒性活性大于他莫昔芬,并且首次与顺铂一样有效。
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Synthesis and preliminary in vitro cytotoxic activity of novel cisplatin and carboplatin analogues.

Six new platinum(II) complexes were synthesized from a common triphenylethylene precursor using various diamines. The cytotoxicity of the compounds, evaluated on human breast cancer cell lines (MCF-7 and MDA-MB-231), was greatly influenced by the nature of the diamine ligand. Two derivatives presented cytotoxic activity greater than tamoxifen and, for the first time, as potent as cisplatin.

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