单核膦配体抗癌 Pt(II) 配合物的氧化：稳定但活性的 Pt(IV) 前药的研究。

Oxidation of anticancer Pt(II) complexes with monodentate phosphane ligands: towards stable but active Pt(IV) prodrugs.

机构信息

Química Inorgánica, Universidad Autónoma de Madrid, 28049 Madrid, Spain.

出版信息

Chem Commun (Camb). 2013 May 25;49(42):4806-8. doi: 10.1039/c3cc38416k.

Abstract

The synthesis, characterization and cytotoxicity studies of two novel platinum(IV) complexes, trans-PtCl4(dma)(PPh3), 1, and trans-PtCl4(ipa)(PPh3), 2, where dma is dimethylamine and ipa is isopropylamine, have been carried out. Both complexes contain aliphatic amines trans to phosphane ligands as a good alternative to take advantage of the phosphane group lipophilicity and the stability of platinum(IV) to obtain more effective drugs. Moreover, the complexes are stable in solution and such stability allowed their antitumoral action and DNA interaction to be checked and proved.

摘要

已对两种新型铂（IV）配合物[trans-PtCl4(dma)(PPh3)]，1 和[trans-PtCl4(ipa)(PPh3)]，2（其中 dma 是二甲胺，ipa 是异丙胺）的合成、表征和细胞毒性研究进行了研究。这两种配合物都含有与膦配体反式的脂族胺，这是利用膦基团亲脂性和铂（IV）的稳定性来获得更有效的药物的一种很好的选择。此外，这些配合物在溶液中稳定，这种稳定性使它们的抗肿瘤作用和 DNA 相互作用得以检查和证明。