Venkatesh V, Sadler Peter J
Met Ions Life Sci. 2018 Feb 5;18. doi: 10.1515/9783110470734-009.
This chapter is an overview of recent progress in the design of Pt(IV) prodrugs. These kinetically-inert octahedral prodrugs can be reduced in cancer cells to active squareplanar Pt(II) complexes, for example by intracellular reducing agents such as glutathione or by photoexcitation. The additional axial ligands in Pt(IV) complexes which are released on reduction, allow bioactive molecules to be delivered which can act synergistically with Pt(II) in killing cancer cells, or act as targeting vectors, allow attachment to polymer and nanoparticle delivery systems, or labelling with fluorescent probes. Pt(IV) prodrugs have yet to be approved for clinical use, although some offer the promise of increased efficacy and reduced side effects.
本章概述了铂（IV）前药设计的最新进展。这些动力学惰性的八面体前药可在癌细胞中还原为活性平面正方形铂（II）配合物，例如通过细胞内还原剂如谷胱甘肽或光激发。铂（IV）配合物中还原时释放的额外轴向配体，可递送生物活性分子，这些分子可与铂（II）协同作用杀死癌细胞，或作为靶向载体，实现与聚合物和纳米颗粒递送系统的连接，或用荧光探针进行标记。尽管一些铂（IV）前药有望提高疗效并减少副作用，但尚未获批用于临床。
